5-HT receptor
Encyclopedia
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G protein-coupled receptor
G protein-coupled receptors , also known as seven-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein-linked receptors , comprise a large protein family of transmembrane receptors that sense molecules outside the cell and activate inside signal...
) and ligand-gated ion channels (LGICs
Ligand-gated ion channel
Ligand-gated ion channels are one type of ionotropic receptor or channel-linked receptor. They are a group of transmembrane ion channels that are opened or closed in response to the binding of a chemical messenger , such as a neurotransmitter.The binding site of endogenous ligands on LGICs...
) found in the central
Central nervous system
The central nervous system is the part of the nervous system that integrates the information that it receives from, and coordinates the activity of, all parts of the bodies of bilaterian animals—that is, all multicellular animals except sponges and radially symmetric animals such as jellyfish...
and peripheral
Peripheral nervous system
The peripheral nervous system consists of the nerves and ganglia outside of the brain and spinal cord. The main function of the PNS is to connect the central nervous system to the limbs and organs. Unlike the CNS, the PNS is not protected by the bone of spine and skull, or by the blood–brain...
nervous systems. They mediate both excitatory and inhibitory neurotransmission. The serotonin receptors are activated by the neurotransmitter
Neurotransmitter
Neurotransmitters are endogenous chemicals that transmit signals from a neuron to a target cell across a synapse. Neurotransmitters are packaged into synaptic vesicles clustered beneath the membrane on the presynaptic side of a synapse, and are released into the synaptic cleft, where they bind to...
serotonin
Serotonin
Serotonin or 5-hydroxytryptamine is a monoamine neurotransmitter. Biochemically derived from tryptophan, serotonin is primarily found in the gastrointestinal tract, platelets, and in the central nervous system of animals including humans...
, which acts as their natural ligand
Ligand (biochemistry)
In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose. In a narrower sense, it is a signal triggering molecule, binding to a site on a target protein.The binding occurs by intermolecular forces, such as ionic bonds, hydrogen...
.
The serotonin receptors modulate the release of many neurotransmitters, including glutamate
Glutamic acid
Glutamic acid is one of the 20 proteinogenic amino acids, and its codons are GAA and GAG. It is a non-essential amino acid. The carboxylate anions and salts of glutamic acid are known as glutamates...
, GABA
Gamma-aminobutyric acid
γ-Aminobutyric acid is the chief inhibitory neurotransmitter in the mammalian central nervous system. It plays a role in regulating neuronal excitability throughout the nervous system...
, dopamine
Dopamine
Dopamine is a catecholamine neurotransmitter present in a wide variety of animals, including both vertebrates and invertebrates. In the brain, this substituted phenethylamine functions as a neurotransmitter, activating the five known types of dopamine receptors—D1, D2, D3, D4, and D5—and their...
, epinephrine
Epinephrine
Epinephrine is a hormone and a neurotransmitter. It increases heart rate, constricts blood vessels, dilates air passages and participates in the fight-or-flight response of the sympathetic nervous system. In chemical terms, adrenaline is one of a group of monoamines called the catecholamines...
/ norepinephrine
Norepinephrine
Norepinephrine is the US name for noradrenaline , a catecholamine with multiple roles including as a hormone and a neurotransmitter...
, and acetylcholine
Acetylcholine
The chemical compound acetylcholine is a neurotransmitter in both the peripheral nervous system and central nervous system in many organisms including humans...
, as well as many hormones, including oxytocin
Oxytocin
Oxytocin is a mammalian hormone that acts primarily as a neuromodulator in the brain.Oxytocin is best known for its roles in sexual reproduction, in particular during and after childbirth...
, prolactin
Prolactin
Prolactin also known as luteotropic hormone is a protein that in humans is encoded by the PRL gene.Prolactin is a peptide hormone discovered by Henry Friesen...
, vasopressin
Vasopressin
Arginine vasopressin , also known as vasopressin, argipressin or antidiuretic hormone , is a neurohypophysial hormone found in most mammals, including humans. Vasopressin is a peptide hormone that controls the reabsorption of molecules in the tubules of the kidneys by affecting the tissue's...
, cortisol
Cortisol
Cortisol is a steroid hormone, more specifically a glucocorticoid, produced by the adrenal gland. It is released in response to stress and a low level of blood glucocorticoids. Its primary functions are to increase blood sugar through gluconeogenesis; suppress the immune system; and aid in fat,...
, corticotropin, and substance P
Substance P
In the field of neuroscience, substance P is a neuropeptide: an undecapeptide that functions as a neurotransmitter and as a neuromodulator. It belongs to the tachykinin neuropeptide family. Substance P and its closely related neuropeptide neurokinin A are produced from a polyprotein precursor...
, among others. The serotonin receptors influence various biological and neurological processes such as aggression, anxiety, appetite, cognition
Cognition
In science, cognition refers to mental processes. These processes include attention, remembering, producing and understanding language, solving problems, and making decisions. Cognition is studied in various disciplines such as psychology, philosophy, linguistics, and computer science...
, learning, memory, mood
Mood (psychology)
A mood is a relatively long lasting emotional state. Moods differ from emotions in that they are less specific, less intense, and less likely to be triggered by a particular stimulus or event....
, nausea, sleep, and thermoregulation
Thermoregulation
Thermoregulation is the ability of an organism to keep its body temperature within certain boundaries, even when the surrounding temperature is very different...
. The serotonin receptors are the target of a variety of pharmaceutical and illicit drugs, including many antidepressant
Antidepressant
An antidepressant is a psychiatric medication used to alleviate mood disorders, such as major depression and dysthymia and anxiety disorders such as social anxiety disorder. According to Gelder, Mayou &*Geddes people with a depressive illness will experience a therapeutic effect to their mood;...
s, antipsychotic
Antipsychotic
An antipsychotic is a tranquilizing psychiatric medication primarily used to manage psychosis , particularly in schizophrenia and bipolar disorder. A first generation of antipsychotics, known as typical antipsychotics, was discovered in the 1950s...
s, anorectic
Anorectic
An anorectic or anorexic , also known as anorexigenic or appetite suppressant, is a dietary supplement and/or drug which reduces appetite, food consumption, and as a result, causes weight loss to occur.-List of anorectics:Numerous pharmaceutical compounds are marketed as appetite suppressants.The...
s, antiemetic
Antiemetic
An antiemetic is a drug that is effective against vomiting and nausea. Antiemetics are typically used to treat motion sickness and the side effects of opioid analgesics, general anaesthetics, and chemotherapy directed against cancer....
s, gastroprokinetic agents, antimigraine agents
Antimigraine
An antimigraine drug is a medication intended to reduce the effects or intensity of migraine headache.Examples are the triptans, including zolmitriptan....
, hallucinogens, and entactogens
Empathogen-entactogen
The terms empathogen and entactogen are used to describe a class of psychoactive drugs that produce distinctive emotional and social effects similar to those of MDMA. Putative members of this class include 2C-B, 2C-I, MDMA, MDA, MDEA, MBDB, 2C-T-7, and 2C-T-2, among others...
.
Classification
With the exception of the 5-HT3 receptor5-HT3 receptor
The 5-HT3 receptor is a member of the superfamily of ligand-gated ion channels, a superfamily that also includes the neuronal nicotinic acetylcholine receptors , and the inhibitory neurotransmitter receptors for GABA and glycine...
, a ligand-gated ion channel
Ligand-gated ion channel
Ligand-gated ion channels are one type of ionotropic receptor or channel-linked receptor. They are a group of transmembrane ion channels that are opened or closed in response to the binding of a chemical messenger , such as a neurotransmitter.The binding site of endogenous ligands on LGICs...
, all other serotonin receptors are G protein-coupled receptor
G protein-coupled receptor
G protein-coupled receptors , also known as seven-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein-linked receptors , comprise a large protein family of transmembrane receptors that sense molecules outside the cell and activate inside signal...
s that activate an intracellular
Intracellular
Not to be confused with intercellular, meaning "between cells".In cell biology, molecular biology and related fields, the word intracellular means "inside the cell".It is used in contrast to extracellular...
second messenger cascade to produce an excitatory or inhibitory response.
Families
| Family | Type | Mechanism | Potential >- | 5-HT1 |
Gi/Go Gi alpha subunit Gi alpha subunit is a heterotrimeric G protein subunit that inhibits the production of cAMP from ATP.- Receptors :The following G protein-coupled receptors couple to the Gi subunit:* Acetylcholine M2 & M4 receptors... -protein coupled. |
Decreasing cellular levels of cAMP Cyclic adenosine monophosphate Cyclic adenosine monophosphate is a second messenger important in many biological processes... . |
>- | Gq/G11-protein coupled. | Increasing cellular levels of IP3 and DAG Diglyceride A diglyceride, or a diacylglycerol , is a glyceride consisting of two fatty acid chains covalently bonded to a glycerol molecule through ester linkages.... . |
>- | Ligand-gated Na+ Sodium Sodium is a chemical element with the symbol Na and atomic number 11. It is a soft, silvery-white, highly reactive metal and is a member of the alkali metals; its only stable isotope is 23Na. It is an abundant element that exists in numerous minerals, most commonly as sodium chloride... and K+ Potassium Potassium is the chemical element with the symbol K and atomic number 19. Elemental potassium is a soft silvery-white alkali metal that oxidizes rapidly in air and is very reactive with water, generating sufficient heat to ignite the hydrogen emitted in the reaction.Potassium and sodium are... cation channel. |
Depolarizing Depolarization In biology, depolarization is a change in a cell's membrane potential, making it more positive, or less negative. In neurons and some other cells, a large enough depolarization may result in an action potential... plasma membrane. |
>- | Gs-protein coupled. | Increasing cellular levels of cAMP Cyclic adenosine monophosphate Cyclic adenosine monophosphate is a second messenger important in many biological processes... . |
>- | Gi/Go Gi alpha subunit Gi alpha subunit is a heterotrimeric G protein subunit that inhibits the production of cAMP from ATP.- Receptors :The following G protein-coupled receptors couple to the Gi subunit:* Acetylcholine M2 & M4 receptors... -protein coupled. |
Decreasing cellular levels of cAMP Cyclic adenosine monophosphate Cyclic adenosine monophosphate is a second messenger important in many biological processes... . |
Inhibitory |
| 5-HT6 | Gs-protein coupled. | Increasing cellular levels of cAMP Cyclic adenosine monophosphate Cyclic adenosine monophosphate is a second messenger important in many biological processes... . |
>- | Gs-protein coupled. | Increasing cellular levels of cAMP Cyclic adenosine monophosphate Cyclic adenosine monophosphate is a second messenger important in many biological processes... . |
Excitatory |
Subtypes
Within these general classes of serotonin receptors, a number of specific types have been characterized:| Overview of Serotonin Receptors | |||||
| Receptor | Gene(s) | Distribution | Function | Agonist Agonist An agonist is a chemical that binds to a receptor of a cell and triggers a response by that cell. Agonists often mimic the action of a naturally occurring substance... s |
Antagonist Receptor antagonist A receptor antagonist is a type of receptor ligand or drug that does not provoke a biological response itself upon binding to a receptor, but blocks or dampens agonist-mediated responses... s |
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| 5-HT1A 5-HT1A receptor The 5-HT1A receptor is a subtype of 5-HT receptor that binds the endogenous neurotransmitter serotonin . It is a G protein-coupled receptor that is coupled to Gi/Go and mediates inhibitory neurotransmission... |
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5-Carboxamidotryptamine 5-Carboxamidotryptamine is a tryptamine derivative closely related to the neurotransmitter serotonin.5-CT acts as a non-selective, high-affinity full agonist at the 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5A, and 5-HT7 receptors, as well as at the 5-HT2, 5-HT3, 5-HT6 receptors with lower affinity. It has... 8-OH-DPAT 8-OH-DPAT is a research chemical of the aminotetralin chemical class which was developed in the 1980s and has been widely used to study the function of the 5-HT1A receptor... Aripiprazole Aripiprazole is an atypical antipsychotic and antidepressant used in the treatment of schizophrenia, bipolar disorder, and clinical depression... Buspirone Buspirone is an anxiolytic psychoactive drug of the azapirone chemical class, and is primarily used to treat generalized anxiety disorder Bristol-Myers Squibb gained FDA approval of buspirone in 1986 for treatment of GAD... (anxiolytic Anxiolytic An anxiolytic is a drug used for the treatment of anxiety, and its related psychological and physical symptoms... and antidepressant Antidepressant An antidepressant is a psychiatric medication used to alleviate mood disorders, such as major depression and dysthymia and anxiety disorders such as social anxiety disorder. According to Gelder, Mayou &*Geddes people with a depressive illness will experience a therapeutic effect to their mood;... ) Cannabidiol Cannabidiol is a cannabinoid found in Cannabis. It is a major constituent of the plant, representing up to 40% in its extracts.It has displayed sedative effects in animal tests... Clozapine Clozapine is an antipsychotic medication used in the treatment of schizophrenia, and is also used off-label in the treatment of bipolar disorder. Wyatt. R and Chew... Dihydroergotamine Dihydroergotamine is an ergot alkaloid used to treat migraines. It is a derivative of ergotamine. It is administered as a nasal spray or injection and has an efficacy similar to that of sumatriptan... Eltoprazine Eltoprazine is a drug of the phenylpiperazine class which is a serenic or antiaggressive agent. It acts as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor. It is closely related to fluprazine and batoprazine, which are similarly acting drugs.... Flesinoxan Flesinoxan is a potent and selective 5-HT1A receptor partial/near-full agonist of the phenylpiperazine class. Originally developed as an antihypertensive agent, it was later found to possess antidepressant and anxiolytic effects in animals... Flibanserin Flibanserin is a drug that was investigated by Boehringer Ingelheim as a novel, non-hormonal treatment for pre-menopausal women with Hypoactive Sexual Desire Disorder . Development was terminated in October 2010 following a negative report by the U.S... Gepirone Gepirone is a psychoactive drug and research chemical of the piperazine and azapirone chemical classes. It is currently under clinical development in an extended release form as an anxiolytic and antidepressant agent... Ipsapirone Ipsapirone is a selective 5-HT1A receptor partial agonist of the piperazine and azapirone chemical classes. It has antidepressant and anxiolytic effects.- References :... Methysergide Methysergide is a prescription drug used for prophylaxis of migraine headaches and is sold under the brand names Sansert and Deseril in 2 mg dosages.-Pharmacology:Methysergide interacts with serotonin receptors... Nefazodone Nefazodone is an antidepressant marketed by Bristol-Myers Squibb. Its sale was discontinued in 2003 in some countries due to the rare incidence of hepatotoxicity , which could lead to the need for a liver transplant, or even death. The incidence of severe liver damage is approximately 1 in every... Psilocin Psilocin , an aromatic compound, sometimes also spelled psilocine, psilocyn, or psilotsin, is a psychedelic mushroom alkaloid. It is found in most psychedelic mushrooms together with its phosphorylated counterpart psilocybin... Quetiapine Quetiapine , is an atypical antipsychotic approved for the treatment of schizophrenia, and bipolar disorder.... Tandospirone Tandospirone , also known as metanopirone, is an anxiolytic and antidepressant used in China and Japan, where it is marketed by Dainippon Sumitomo Pharma... Trazodone Trazodone is an antidepressant of the serotonin antagonist and reuptake inhibitor class. It is a phenylpiperazine compound... Urapidil Urapidil is a sympatholytic antihypertensive drug. It acts as an α1-adrenoceptor antagonist and as an 5-HT1A receptor agonist Although an initial report suggested that urapidil was also an α2-adrenoceptor agonist, this was not substantiated in later studies that demonstrated it was devoid of... Xaliproden Xaliproden is a drug which acts as a 5HT1A agonist. It has neurotrophic and neuroprotective effects in vitro, and has been proposed for use in the treatment of several neurodegenerative conditions including amyotrophic lateral sclerosis and Alzheimer's disease.Development of xaliproden for these... Yohimbine Yohimbine is an alkaloid with stimulant and aphrodisiac effects found naturally in Pausinystalia yohimbe . It is also found naturally in Rauwolfia serpentina , Alchornea floribunda , along with several other active alkaloids... Ziprasidone Ziprasidone was the fifth atypical antipsychotic to gain FDA approval . In the United States, Ziprasidone is Food and Drug Administration approved for the treatment of schizophrenia, and the intramuscular injection form of ziprasidone is approved for acute agitation in schizophrenic patients... |
Alprenolol Alprenolol, or alfeprol, alpheprol, and alprenololum , is a non-selective beta blocker as well as 5-HT1A receptor antagonist, used in the treatment of angina pectoris... Asenapine Asenapine is a new atypical antipsychotic developed for the treatment of schizophrenia and acute mania associated with bipolar disorder by Schering-Plough after its November 19, 2007 merger with Organon International. Development of the drug, through Phase III trials, began while Organon was still... Cyanopindolol Cyanopindolol is a drug related to pindolol which acts as both a β1 adrenoreceptor antagonist and a 5-HT1A receptor antagonist. Its radiolabelled derivative iodocyanopindolol has been widely used in mapping the distribution of beta adrenoreceptors in the body.... Iodocyanopindolol Iodocyanopindolol is a drug related to pindolol which acts as both a β1 adrenoreceptor antagonist and a 5-HT1A receptor antagonist. Its 125I radiolabelled derivative has been widely used in mapping the distribution of beta adrenoreceptors in the body.... Lecozotan Lecozotan is an investigational drug by Wyeth tested for improvement of cognitive functions of Alzheimer's disease patients., the first Phase III clinical trial has been completed.- Method of action :... NAN-190 NAN-190 is a drug and research chemical widely used in scientific studies. It was previously believed to act as a selective 5-HT1A receptor antagonist, but a subsequent discovery showed that it also potently blocks the α2-adrenergic receptor. The new finding has raised significant concerns about... Nebivolol Nebivolol is a β1 receptor blocker with nitric oxide-potentiating vasodilatory effect used in treatment of hypertension and, in Europe, also for left ventricular failure... Oxprenolol Oxprenolol is a non-selective beta blocker with some intrinsic sympathomimetic activity... Pindolol Pindolol is a beta blocker.... Robalzotan Robalzotan is a selective antagonist at the 5-HT1A receptor. It was shown to completely reverse the autoreceptor-mediated inhibition of serotonin release induced by the administration of selective serotonin reuptake inhibitors like citalopram in rodent studies... Spiperone Spiperone is a psychoactive drug and research chemical belonging to the butyrophenone chemical class. It functions as a 5-HT1A, 5-HT2A, 5-HT7, and D2 receptor antagonist, and has been used to identify these receptors when labeled with tritium. It has negligible affinity for the 5-HT2C receptor... UH-301 UH-301 is a drug and research chemical widely used in scientific studies. It acts as a selective 5-HT1A receptor silent antagonist. It is structurally related to 8-OH-DPAT.... WAY-100,135 WAY-100,135 is a piperazine drug and research chemical used in scientific studies. It was originally believed to act as a selective 5-HT1A receptor antagonist, but subsequent research demonstrated that it also acts as a partial agonist at the 5-HT1B and 5-HT1D receptors.... |
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| 5-HT1B 5-HT1B receptor 5-hydroxytryptamine receptor 1B also known as the 5-HT1B receptor is a protein that in humans is encoded by the HTR1B gene. The 5-HT1B receptor is a 5-HT receptor subtype.-Tissue distribution and function:... |
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5-Carboxamidotryptamine 5-Carboxamidotryptamine is a tryptamine derivative closely related to the neurotransmitter serotonin.5-CT acts as a non-selective, high-affinity full agonist at the 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5A, and 5-HT7 receptors, as well as at the 5-HT2, 5-HT3, 5-HT6 receptors with lower affinity. It has... CP-93,129 CP-93,129 is a drug which acts as a potent and selective serotonin 5-HT1B receptor agonist, with approximately 150x and 200x selectivity over the closely related 5-HT1D and 5-HT1A receptors. It is used in the study of 5-HT1B receptors in the brain, particularly their role in modulating the release... CP-94,253 CP-94,253 is a drug which acts as a potent and selective serotonin 5-HT1B receptor agonist, with approximately 25x and 40x selectivity over the closely related 5-HT1D and 5-HT1A receptors... Dihydroergotamine Dihydroergotamine is an ergot alkaloid used to treat migraines. It is a derivative of ergotamine. It is administered as a nasal spray or injection and has an efficacy similar to that of sumatriptan... Eltoprazine Eltoprazine is a drug of the phenylpiperazine class which is a serenic or antiaggressive agent. It acts as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor. It is closely related to fluprazine and batoprazine, which are similarly acting drugs.... Methysergide Methysergide is a prescription drug used for prophylaxis of migraine headaches and is sold under the brand names Sansert and Deseril in 2 mg dosages.-Pharmacology:Methysergide interacts with serotonin receptors... Antimigraine An antimigraine drug is a medication intended to reduce the effects or intensity of migraine headache.Examples are the triptans, including zolmitriptan.... )
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Alprenolol Alprenolol, or alfeprol, alpheprol, and alprenololum , is a non-selective beta blocker as well as 5-HT1A receptor antagonist, used in the treatment of angina pectoris... AR-A000002 AR-A000002 is a drug which is one of the first compounds developed to act as a selective antagonist for the serotonin receptor 5-HT1B, with approximately 10x selectivity for 5-HT1B over the closely related 5-HT1D receptor. It has been shown to produce sustained increases in levels of serotonin in... Asenapine Asenapine is a new atypical antipsychotic developed for the treatment of schizophrenia and acute mania associated with bipolar disorder by Schering-Plough after its November 19, 2007 merger with Organon International. Development of the drug, through Phase III trials, began while Organon was still... Cyanopindolol Cyanopindolol is a drug related to pindolol which acts as both a β1 adrenoreceptor antagonist and a 5-HT1A receptor antagonist. Its radiolabelled derivative iodocyanopindolol has been widely used in mapping the distribution of beta adrenoreceptors in the body.... Iodocyanopindolol Iodocyanopindolol is a drug related to pindolol which acts as both a β1 adrenoreceptor antagonist and a 5-HT1A receptor antagonist. Its 125I radiolabelled derivative has been widely used in mapping the distribution of beta adrenoreceptors in the body.... Isamoltane Isamoltane is a drug used in scientific research. It acts as an antagonist at the β-adrenergic, 5-HT1A, and 5-HT1B receptors. It has about five times the potency for the 5-HT1B receptor over the 5-HT1A receptor . It has anxiolytic effects in rodents.... Metergoline Metergoline is a psychoactive drug of the ergoline chemical class which acts as a ligand for various serotonin and dopamine receptors.... Oxprenolol Oxprenolol is a non-selective beta blocker with some intrinsic sympathomimetic activity... Pindolol Pindolol is a beta blocker.... SB-216,641 SB-216,641 is a drug which is a selective antagonist for the serotonin receptor 5-HT1B, with around 25x selectivity over the closely related 5-HT1D receptor. It is used in scientific research, and has demonstrated anxiolytic effects in animal studies.... Yohimbine Yohimbine is an alkaloid with stimulant and aphrodisiac effects found naturally in Pausinystalia yohimbe . It is also found naturally in Rauwolfia serpentina , Alchornea floribunda , along with several other active alkaloids... |
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| 5-HT1D 5-HT1D receptor 5-hydroxytryptamine receptor 1D, also known as HTR1D, is a 5-HT receptor, but also denotes the human gene encoding it. 5-HT1D acts on the central nervous system, and affects locomotion and anxiety... |
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5-Carboxamidotryptamine 5-Carboxamidotryptamine is a tryptamine derivative closely related to the neurotransmitter serotonin.5-CT acts as a non-selective, high-affinity full agonist at the 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5A, and 5-HT7 receptors, as well as at the 5-HT2, 5-HT3, 5-HT6 receptors with lower affinity. It has... Dihydroergotamine Dihydroergotamine is an ergot alkaloid used to treat migraines. It is a derivative of ergotamine. It is administered as a nasal spray or injection and has an efficacy similar to that of sumatriptan... Methysergide Methysergide is a prescription drug used for prophylaxis of migraine headaches and is sold under the brand names Sansert and Deseril in 2 mg dosages.-Pharmacology:Methysergide interacts with serotonin receptors... Antimigraine An antimigraine drug is a medication intended to reduce the effects or intensity of migraine headache.Examples are the triptans, including zolmitriptan.... )
Yohimbine Yohimbine is an alkaloid with stimulant and aphrodisiac effects found naturally in Pausinystalia yohimbe . It is also found naturally in Rauwolfia serpentina , Alchornea floribunda , along with several other active alkaloids... |
BRL-15572 BRL-15,572 is a drug which acts as a selective antagonist for the serotonin receptor subtype 5-HT1D, with around 60x selectivity over other related receptors... Ketanserin Ketanserin is a drug with affinity for multiple G protein-coupled receptors . Initially it was believed to be a highly selective antagonist for serotonin 5-HT2A receptors, however this is not true. Ketanserin only has moderate selectivity for 5-HT2A receptors over 5-HT2C receptors... Metergoline Metergoline is a psychoactive drug of the ergoline chemical class which acts as a ligand for various serotonin and dopamine receptors.... Rauwolscine Rauwolscine, also known as isoyohimbine, α-yohimbine, and corynanthidine, is an alkaloid found in various species within the genera Rauwolfia and Pausinystalia . It is a stereoisomer of yohimbine... Ritanserin Ritanserin is a serotonin antagonist with possibilities for the treatment of many neurological disorders.When used together with typical antipsychotics in the treatment of schizophrenia is able to decrease negative symptoms and adds some "atypicality" as parkinsonism is slightly decreased.-... |
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Eletriptan Eletriptan is a second generation triptan drug marketed and manufactured by Pfizer Inc for the treatment of migraine headaches. It is sold in the US under the brand name Relpax.-Approval and availability:... Methysergide Methysergide is a prescription drug used for prophylaxis of migraine headaches and is sold under the brand names Sansert and Deseril in 2 mg dosages.-Pharmacology:Methysergide interacts with serotonin receptors... Tryptamine Tryptamine is a monoamine alkaloid found in plants, fungi, and animals. It is based around the indole ring structure, and is chemically related to the amino acid tryptophan, from which its name is derived... |
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| 5-HT2A 5-HT2A receptor The mammalian 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and is a G protein-coupled receptor . This is the main excitatory receptor subtype among the GPCRs for serotonin , although 5-HT2A may also have an inhibitory effect on certain areas such... |
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2C-B 2C-B or 4-bromo-2,5-dimethoxyphenethylamine is a psychedelic drug of the 2C family. It was first synthesized by Alexander Shulgin in 1974. In Shulgin's book PiHKAL, the dosage range is listed as 16–24 mg. 2C-B is sold as a white powder sometimes pressed in tablets or gel caps and is referred... 5-MeO-DMT 5-MeO-DMT is a powerful psychedelic tryptamine. It is found in a wide variety of plant and psychoactive toad species and, like its close relatives DMT and bufotenin , it has been used as an entheogen by South American shamans for thousands of years.-Chemistry:5-MeO-DMT was first synthesized in... Benzylpiperazine Benzylpiperazine is a recreational drug with euphoric, stimulant properties. The effects produced by BZP are comparable to those produced by amphetamine. Adverse effects have been reported following its use including acute psychosis, renal toxicity, and seizures... Bufotenin Bufotenin , or 5-hydroxy-dimethyltryptamine , is a tryptamine related to the neurotransmitter serotonin... Dimethyltryptamine N,N-Dimethyltryptamine is a naturally occurring psychedelic compound of the tryptamine family. DMT is found in several plants, and also in trace amounts in humans and other mammals, where it is originally derived from the essential amino acid tryptophan, and ultimately produced by the enzyme INMT... 2,5-Dimethoxy-4-methylamphetamine 2,5-Dimethoxy-4-methylamphetamine is a psychedelic and a substituted amphetamine... Ergonovine Ergometrine , is an ergoline derivative, and one of the primary ergot and morning glory alkaloids... Lisuride Lisuride is an antiparkinson agent of the iso-ergoline class, chemically related to the dopaminergic ergoline Parkinson's drugs. Lisuride is described as free base and as hydrogen maleate salt.Lisuride is used to lower prolactin and, in low doses, to prevent migraine attacks... LSD Lysergic acid diethylamide, abbreviated LSD or LSD-25, also known as lysergide and colloquially as acid, is a semisynthetic psychedelic drug of the ergoline family, well known for its psychological effects which can include altered thinking processes, closed and open eye visuals, synaesthesia, an... Mescaline Mescaline or 3,4,5-trimethoxyphenethylamine is a naturally occurring psychedelic alkaloid of the phenethylamine class used mainly as an entheogen.... Myristicin Myristicin is a phenylpropene, a natural organic compound present in small amounts in the essential oil of nutmeg and to a lesser extent in other spices such as parsley and dill.It is insoluble in water, but soluble in ethanol and acetone.-Uses:... Psilocin Psilocin , an aromatic compound, sometimes also spelled psilocine, psilocyn, or psilotsin, is a psychedelic mushroom alkaloid. It is found in most psychedelic mushrooms together with its phosphorylated counterpart psilocybin... Psilocybin Psilocybin is a naturally occurring psychedelic prodrug, with mind-altering effects similar to those of LSD and mescaline, after it is converted to psilocin. The effects can include altered thinking processes, perceptual distortions, an altered sense of time, and spiritual experiences, as well as... Yohimbine Yohimbine is an alkaloid with stimulant and aphrodisiac effects found naturally in Pausinystalia yohimbe . It is also found naturally in Rauwolfia serpentina , Alchornea floribunda , along with several other active alkaloids... |
Atypical antipsychotic The atypical antipsychotics are a group of antipsychotic tranquilizing drugs used to treat psychiatric conditions. Some atypical antipsychotics are FDA approved for use in the treatment of schizophrenia... s
Aripiprazole Aripiprazole is an atypical antipsychotic and antidepressant used in the treatment of schizophrenia, bipolar disorder, and clinical depression... Asenapine Asenapine is a new atypical antipsychotic developed for the treatment of schizophrenia and acute mania associated with bipolar disorder by Schering-Plough after its November 19, 2007 merger with Organon International. Development of the drug, through Phase III trials, began while Organon was still... Amitriptyline Amitriptyline is a tricyclic antidepressant . It is the most widely used TCA and has at least equal efficacy against depression as the newer class of SSRIs... Clomipramine Clomipramine is a tricyclic antidepressant . It was developed in the 1960s by the Swiss drug manufacturer Geigy and has been in clinical use worldwide ever since.- Indications :... Cyproheptadine Cyproheptadine , sold under the brand name Periactin, is a first-generation antihistamine with additional anticholinergic, antiserotonergic, and local anesthetic properties.- Indications :... Eplivanserin Eplivanserin was an experimental drug for the treatment of insomnia which was being developed by Sanofi Aventis.... Etoperidone Etoperidone , also known as clopradone and thozalinone, is an antidepressant of the phenylpiperazine class which was introduced in Europe in 1977... Iloperidone Iloperidone, also known as Fanapt, Fanapta, and previously known as Zomaril, is an atypical antipsychotic for the treatment of schizophrenia. It was approved by the U.S... Ketanserin Ketanserin is a drug with affinity for multiple G protein-coupled receptors . Initially it was believed to be a highly selective antagonist for serotonin 5-HT2A receptors, however this is not true. Ketanserin only has moderate selectivity for 5-HT2A receptors over 5-HT2C receptors... (antihypertensive Antihypertensive The antihypertensives are a class of drugs that are used to treat hypertension . Evidence suggests that reduction of the blood pressure by 5 mmHg can decrease the risk of stroke by 34%, of ischaemic heart disease by 21%, and reduce the likelihood of dementia, heart failure, and mortality from... ) Methysergide Methysergide is a prescription drug used for prophylaxis of migraine headaches and is sold under the brand names Sansert and Deseril in 2 mg dosages.-Pharmacology:Methysergide interacts with serotonin receptors... Mianserin Mianserin is a psychoactive drug of the tetracyclic antidepressant chemical class which is classified as a noradrenergic and specific serotonergic antidepressant and has antidepressant, anxiolytic, hypnotic, antiemetic, orexigenic, and antihistamine effects... Mirtazapine Mirtazapine is a tetracyclic antidepressant used primarily in the treatment of depression. It is also sometimes used as a hypnotic, antiemetic, and appetite stimulant, and for the treatment of anxiety, among other indications... Nefazodone Nefazodone is an antidepressant marketed by Bristol-Myers Squibb. Its sale was discontinued in 2003 in some countries due to the rare incidence of hepatotoxicity , which could lead to the need for a liver transplant, or even death. The incidence of severe liver damage is approximately 1 in every... Pimavanserin Pimavanserin is a drug developed by Acadia Pharmaceuticals which acts as an inverse agonist on the serotonin receptor subtype 5-HT2A, with 10x selectivity over 5-HT2C, and no significant affinity or activity at 5-HT2B or dopamine receptors... Pizotifen Pizotifen or pizotyline , trade name Sandomigran, is a benzocycloheptene based drug used as a medicine, primarily as a preventative to reduce the frequency of recurrent migraine headaches.-Uses:... Ritanserin Ritanserin is a serotonin antagonist with possibilities for the treatment of many neurological disorders.When used together with typical antipsychotics in the treatment of schizophrenia is able to decrease negative symptoms and adds some "atypicality" as parkinsonism is slightly decreased.-... Trazodone Trazodone is an antidepressant of the serotonin antagonist and reuptake inhibitor class. It is a phenylpiperazine compound... |
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| 5-HT2B 5-HT2B receptor 5-hydroxytryptamine receptor 2B, also known as HTR2B, is a 5-HT2 receptor, but also denotes the human gene encoding it.-Function:... |
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BW-723C86 BW-723C86 is a tryptamine derivative drug which acts as a 5-HT2B receptor agonist. It has anxiolytic effects in animal studies, and is also used for investigating the function of the 5-HT2B receptor in a range of other tissues.... Fenfluramine Fenfluramine is a drug that was part of the Fen-Phen anti-obesity medication . Fenfluramine was introduced on the U.S. market in 1973. It is the racemic mixture of two enantiomers, dextrofenfluramine and levofenfluramine... Norfenfluramine Norfenfluramine is a psychoactive drug which functions as a serotonin releasing agent and potent 5HT2B receptor agonist. The action of norfenfluramine on 5HT2B receptors on heart valves leads to a characteristic pattern of heart failure following proliferation of cardiac fibroblasts on the... Ro60-0175 Ro60-0175 is a drug developed by Hoffmann–La Roche, which has applications in scientific research. It acts as a potent and selective agonist for both the 5-HT2B and 5-HT2C serotonin receptor subtypes, with good selectivity over the closely related 5-HT2A subtype, and little or no affinity at other... |
Asenapine Asenapine is a new atypical antipsychotic developed for the treatment of schizophrenia and acute mania associated with bipolar disorder by Schering-Plough after its November 19, 2007 merger with Organon International. Development of the drug, through Phase III trials, began while Organon was still... Benzylpiperazine Benzylpiperazine is a recreational drug with euphoric, stimulant properties. The effects produced by BZP are comparable to those produced by amphetamine. Adverse effects have been reported following its use including acute psychosis, renal toxicity, and seizures... Ketanserin Ketanserin is a drug with affinity for multiple G protein-coupled receptors . Initially it was believed to be a highly selective antagonist for serotonin 5-HT2A receptors, however this is not true. Ketanserin only has moderate selectivity for 5-HT2A receptors over 5-HT2C receptors... Methysergide Methysergide is a prescription drug used for prophylaxis of migraine headaches and is sold under the brand names Sansert and Deseril in 2 mg dosages.-Pharmacology:Methysergide interacts with serotonin receptors... Ritanserin Ritanserin is a serotonin antagonist with possibilities for the treatment of many neurological disorders.When used together with typical antipsychotics in the treatment of schizophrenia is able to decrease negative symptoms and adds some "atypicality" as parkinsonism is slightly decreased.-... Tegaserod Tegaserod is a 5-HT4 agonist manufactured by Novartis and sold under the name Zelnorm for the management of irritable bowel syndrome and constipation. Approved by the FDA in 2002, it was subsequently removed from the market in 2007 due to FDA concerns about possible adverse cardiovascular effects... Yohimbine Yohimbine is an alkaloid with stimulant and aphrodisiac effects found naturally in Pausinystalia yohimbe . It is also found naturally in Rauwolfia serpentina , Alchornea floribunda , along with several other active alkaloids... |
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| 5-HT2C 5-HT2C receptor The 5-HT2C receptor is a subtype of 5-HT receptor that binds the endogenous neurotransmitter serotonin . It is a G protein-coupled receptor that is coupled to Gq/G11 and mediates excitatory neurotransmission. HTR2C denotes the human gene encoding for the receptor, that in humans is located at the... |
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A-372,159 A-372,159 is a drug which acts as a potent and selective partial agonist for the 5HT2C receptor, with more than 100x selectivity over the closely related 5-HT2B receptor and a Ki of 3nM. It has been found to produce anorectic effects in animal studies and produced significant weight loss in rats... AL-38022A AL-38022A is an indazole derivative drug which is one of a range of similar drugs developed for scientific research and with some possible clinical applications. It acts as a potent and selective agonist for the 5-HT2 family of serotonin receptors, with highest binding affinity for the 5-HT2C... Aripiprazole Aripiprazole is an atypical antipsychotic and antidepressant used in the treatment of schizophrenia, bipolar disorder, and clinical depression... Ergonovine Ergometrine , is an ergoline derivative, and one of the primary ergot and morning glory alkaloids... Lorcaserin Lorcaserin is a weight-loss drug developed by Arena Pharmaceuticals. It has serotonergic properties and acts as an anorectic. On 22 December 2009 a New Drug Application was submitted to the Food and Drug Administration in the United States and lorcaserin is pending approval... Ro60-0175 Ro60-0175 is a drug developed by Hoffmann–La Roche, which has applications in scientific research. It acts as a potent and selective agonist for both the 5-HT2B and 5-HT2C serotonin receptor subtypes, with good selectivity over the closely related 5-HT2A subtype, and little or no affinity at other... Trazodone Trazodone is an antidepressant of the serotonin antagonist and reuptake inhibitor class. It is a phenylpiperazine compound... (hypnotic Hypnotic Hypnotic drugs are a class of psychoactives whose primary function is to induce sleep and to be used in the treatment of insomnia and in surgical anesthesia... ) YM-348 YM-348 is an indazole derivative drug which acts as a potent and selective 5-HT2C receptor agonist, with an EC50 of 1nM and 15x selectivity over 5-HT2A, although it only has moderate selectivity of 3x over the closely related 5-HT2B receptor. It has thermogenic and anorectic effects in animal... |
Antidepressant An antidepressant is a psychiatric medication used to alleviate mood disorders, such as major depression and dysthymia and anxiety disorders such as social anxiety disorder. According to Gelder, Mayou &*Geddes people with a depressive illness will experience a therapeutic effect to their mood;... ) Amitriptyline Amitriptyline is a tricyclic antidepressant . It is the most widely used TCA and has at least equal efficacy against depression as the newer class of SSRIs... Asenapine Asenapine is a new atypical antipsychotic developed for the treatment of schizophrenia and acute mania associated with bipolar disorder by Schering-Plough after its November 19, 2007 merger with Organon International. Development of the drug, through Phase III trials, began while Organon was still... Clomipramine Clomipramine is a tricyclic antidepressant . It was developed in the 1960s by the Swiss drug manufacturer Geigy and has been in clinical use worldwide ever since.- Indications :... Clozapine Clozapine is an antipsychotic medication used in the treatment of schizophrenia, and is also used off-label in the treatment of bipolar disorder. Wyatt. R and Chew... (antipsychotic Antipsychotic An antipsychotic is a tranquilizing psychiatric medication primarily used to manage psychosis , particularly in schizophrenia and bipolar disorder. A first generation of antipsychotics, known as typical antipsychotics, was discovered in the 1950s... ) Cyproheptadine Cyproheptadine , sold under the brand name Periactin, is a first-generation antihistamine with additional anticholinergic, antiserotonergic, and local anesthetic properties.- Indications :... Eltoprazine Eltoprazine is a drug of the phenylpiperazine class which is a serenic or antiaggressive agent. It acts as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor. It is closely related to fluprazine and batoprazine, which are similarly acting drugs.... Etoperidone Etoperidone , also known as clopradone and thozalinone, is an antidepressant of the phenylpiperazine class which was introduced in Europe in 1977... Fluoxetine Fluoxetine is an antidepressant of the selective serotonin reuptake inhibitor class. It is manufactured and marketed by Eli Lilly and Company... Iloperidone Iloperidone, also known as Fanapt, Fanapta, and previously known as Zomaril, is an atypical antipsychotic for the treatment of schizophrenia. It was approved by the U.S... Ketanserin Ketanserin is a drug with affinity for multiple G protein-coupled receptors . Initially it was believed to be a highly selective antagonist for serotonin 5-HT2A receptors, however this is not true. Ketanserin only has moderate selectivity for 5-HT2A receptors over 5-HT2C receptors... (antihypertensive Antihypertensive The antihypertensives are a class of drugs that are used to treat hypertension . Evidence suggests that reduction of the blood pressure by 5 mmHg can decrease the risk of stroke by 34%, of ischaemic heart disease by 21%, and reduce the likelihood of dementia, heart failure, and mortality from... ) Lisuride Lisuride is an antiparkinson agent of the iso-ergoline class, chemically related to the dopaminergic ergoline Parkinson's drugs. Lisuride is described as free base and as hydrogen maleate salt.Lisuride is used to lower prolactin and, in low doses, to prevent migraine attacks... Methysergide Methysergide is a prescription drug used for prophylaxis of migraine headaches and is sold under the brand names Sansert and Deseril in 2 mg dosages.-Pharmacology:Methysergide interacts with serotonin receptors... Mianserin Mianserin is a psychoactive drug of the tetracyclic antidepressant chemical class which is classified as a noradrenergic and specific serotonergic antidepressant and has antidepressant, anxiolytic, hypnotic, antiemetic, orexigenic, and antihistamine effects... Mirtazapine Mirtazapine is a tetracyclic antidepressant used primarily in the treatment of depression. It is also sometimes used as a hypnotic, antiemetic, and appetite stimulant, and for the treatment of anxiety, among other indications... Nefazodone Nefazodone is an antidepressant marketed by Bristol-Myers Squibb. Its sale was discontinued in 2003 in some countries due to the rare incidence of hepatotoxicity , which could lead to the need for a liver transplant, or even death. The incidence of severe liver damage is approximately 1 in every... Olanzapine Olanzapine is an atypical antipsychotic, approved by the FDA for the treatment of schizophrenia and bipolar disorder... Quetiapine Quetiapine , is an atypical antipsychotic approved for the treatment of schizophrenia, and bipolar disorder.... Risperidone Risperidone is a second generation or atypical antipsychotic, sold under the trade name . It is used to treat schizophrenia , schizoaffective disorder, the mixed and manic states associated with bipolar disorder, and irritability in people with autism... Ritanserin Ritanserin is a serotonin antagonist with possibilities for the treatment of many neurological disorders.When used together with typical antipsychotics in the treatment of schizophrenia is able to decrease negative symptoms and adds some "atypicality" as parkinsonism is slightly decreased.-... Trazodone Trazodone is an antidepressant of the serotonin antagonist and reuptake inhibitor class. It is a phenylpiperazine compound... Ziprasidone Ziprasidone was the fifth atypical antipsychotic to gain FDA approval . In the United States, Ziprasidone is Food and Drug Administration approved for the treatment of schizophrenia, and the intramuscular injection form of ziprasidone is approved for acute agitation in schizophrenic patients... |
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| 5-HT3 5-HT3 receptor The 5-HT3 receptor is a member of the superfamily of ligand-gated ion channels, a superfamily that also includes the neuronal nicotinic acetylcholine receptors , and the inhibitory neurotransmitter receptors for GABA and glycine... |
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2-Methyl-5-hydroxytryptamine 2-Methyl-5-hydroxytryptamine is a tryptamine derivative closely related to the neurotransmitter serotonin which acts as a moderately selective full agonist at the 5-HT3 receptor.- See also :... Benzylpiperazine Benzylpiperazine is a recreational drug with euphoric, stimulant properties. The effects produced by BZP are comparable to those produced by amphetamine. Adverse effects have been reported following its use including acute psychosis, renal toxicity, and seizures... Quipazine Quipazine is a piperazine drug used in scientific research. It is a moderately selective serotonin receptor antagonist, binding to a range of different serotonin receptors, but particularly to the 5-HT2A and 5-HT3.... RS-56812 RS-56812 is a potent and selective partial agonist at the 5HT3 receptor. It has been shown to improve performance on animal tests of memory.... |
Alosetron Alosetron is a 5-HT3 antagonist used for the management of severe diarrhea-predominant irritable bowel syndrome in women only. It is currently marketed by Prometheus Laboratories Inc...
Clozapine Clozapine is an antipsychotic medication used in the treatment of schizophrenia, and is also used off-label in the treatment of bipolar disorder. Wyatt. R and Chew... Metoclopramide Metoclopramide is an antiemetic and gastroprokinetic agent. It is commonly used to treat nausea and vomiting, to facilitate gastric emptying in people with gastroparesis, and as a treatment for the gastric stasis often associated with migraine headaches.-Medical uses:Metoclopramide is commonly... Mianserin Mianserin is a psychoactive drug of the tetracyclic antidepressant chemical class which is classified as a noradrenergic and specific serotonergic antidepressant and has antidepressant, anxiolytic, hypnotic, antiemetic, orexigenic, and antihistamine effects... Mirtazapine Mirtazapine is a tetracyclic antidepressant used primarily in the treatment of depression. It is also sometimes used as a hypnotic, antiemetic, and appetite stimulant, and for the treatment of anxiety, among other indications... Olanzapine Olanzapine is an atypical antipsychotic, approved by the FDA for the treatment of schizophrenia and bipolar disorder... Quetiapine Quetiapine , is an atypical antipsychotic approved for the treatment of schizophrenia, and bipolar disorder.... |
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| 5-HT4 5-HT4 receptor 5-hydroxytryptamine receptor 4 is a protein that in humans is encoded by the HTR4 gene.- Location :The receptor is located in the alimentary tract, urinary bladder, heart and adrenal gland as well as the central nervous system .... |
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5-Methoxytryptamine 5-Methoxytryptamine , also known as mexamine, is a tryptamine derivative closely related to the neurotransmitters serotonin and melatonin. 5-MT has been shown to occur naturally in the body in low levels. It is biosynthesized via the deacetylation of melatonin in the pineal gland.5-MT acts as a... Cinitapride Cinitapride is a gastroprokinetic agent and antiulcer agent of the benzamide class which is marketed in India, Mexico, Pakistan and Spain... Cisapride Cisapride is a gastroprokinetic agent, a drug which increases motility in the upper gastrointestinal tract. It acts directly as a serotonin 5-HT4 receptor agonist and indirectly as a parasympathomimetic. Stimulation of the serotonin receptors increases acetylcholine release in the enteric nervous... (gastroprokinetic Prokinetic agent A gastroprokinetic agent, gastrokinetic, or prokinetic, is a type of drug which enhances gastrointestinal motility by increasing the frequency of contractions in the small intestine or making them stronger, but without disrupting their rhythm... ) Dazopride Dazopride is an antiemetic and gastroprokinetic agent of the benzamide class which was never marketed. It acts as a 5-HT3 receptor antagonist and 5-HT4 receptor agonist. In addition to its gastrointestinal effects, dazopride facilitates learning and memory in mice.... Metoclopramide Metoclopramide is an antiemetic and gastroprokinetic agent. It is commonly used to treat nausea and vomiting, to facilitate gastric emptying in people with gastroparesis, and as a treatment for the gastric stasis often associated with migraine headaches.-Medical uses:Metoclopramide is commonly... Mosapride Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist which accelerates gastric emptying and is used for the treatment of acid reflux, irritable bowel syndrome and functional dyspepsia.... Prucalopride Prucalopride is a drug acting as a selective, high affinity 5-HT4 receptor agonist which targets the impaired motility associated with chronic constipation, thus normalising bowel movements... Renzapride Renzapride is a gastroprokinetic agent and antiemetic which acts as a full 5-HT4 full agonist and 5-HT3 antagonist. It also functions as a 5-HT2B antagonist and has some affinity for the 5-HT2A and 5-HT2C receptors, though it is unlikely that these properties contribute to its therapeutic... Tegaserod Tegaserod is a 5-HT4 agonist manufactured by Novartis and sold under the name Zelnorm for the management of irritable bowel syndrome and constipation. Approved by the FDA in 2002, it was subsequently removed from the market in 2007 due to FDA concerns about possible adverse cardiovascular effects... Zacopride Zacopride is a potent antagonist at the 5HT3 receptor and an agonist at the 5HT4 receptor. It has anxiolytic and nootropic effects in animal models, with the enantiomer being the more active form... |
Piboserod Piboserod is a selective 5-HT4 receptor antagonist which was marketed and manufactured by GlaxoSmithKline under the trade name Serlipet for the management of atrial fibrillation and irritable bowel syndrome... |
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| 5-HT5A 5-HT5A receptor 5-hydroxytryptamine receptor 5A, also known as HTR5A, is a protein which in humans is encoded by the HTR5A gene.- Function :... |
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5-Carboxamidotryptamine 5-Carboxamidotryptamine is a tryptamine derivative closely related to the neurotransmitter serotonin.5-CT acts as a non-selective, high-affinity full agonist at the 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5A, and 5-HT7 receptors, as well as at the 5-HT2, 5-HT3, 5-HT6 receptors with lower affinity. It has... Valerenic acid Valerenic acid is a sesquiterpenoid constituent of the essential oil of the Valerian plant. Not to be confused with valeric acid.Valerian is used as a herbal sedative which may be helpful in the treatment of insomnia.... |
Asenapine Asenapine is a new atypical antipsychotic developed for the treatment of schizophrenia and acute mania associated with bipolar disorder by Schering-Plough after its November 19, 2007 merger with Organon International. Development of the drug, through Phase III trials, began while Organon was still... Ritanserin Ritanserin is a serotonin antagonist with possibilities for the treatment of many neurological disorders.When used together with typical antipsychotics in the treatment of schizophrenia is able to decrease negative symptoms and adds some "atypicality" as parkinsonism is slightly decreased.-... SB-699,551 SB-699,551 is a drug which was the first compound developed to act as a selective antagonist for the serotonin receptor 5-HT5A, with selectivity of around 100x over other serotonin receptor subtypes... |
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| 5-HT6 5-HT6 receptor The 5-HT6 receptor is a subtype of 5-HT receptor that binds the endogenous neurotransmitter serotonin . It is a G protein-coupled receptor that is coupled to Gs/Go and mediates excitatory neurotransmission. HTR6 denotes the human gene encoding for the receptor.-Distribution:The 5-HT6 receptor is... |
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EMD-386,088 EMD-386,088 is an indole derivative which is used in scientific research. It acts as a potent and selective 5-HT6 receptor agonist, with a Ki of 1 nM, a significantly higher affinity than older 5-HT6 agonists such as EMDT, although it possesses moderate affinity for the 5-HT3 receptor as well.... 2-Ethyl-5-methoxy-N,N-dimethyltryptamine 2-Ethyl-5-methoxy-N,N-dimethyltryptamine is a tryptamine derivative which is used in scientific research. It acts as a selective 5-HT6 receptor agonist, with a Ki of 16 nM, and was one of the first selective agonists developed for this receptor... |
Amitriptyline Amitriptyline is a tricyclic antidepressant . It is the most widely used TCA and has at least equal efficacy against depression as the newer class of SSRIs... Aripiprazole Aripiprazole is an atypical antipsychotic and antidepressant used in the treatment of schizophrenia, bipolar disorder, and clinical depression... Asenapine Asenapine is a new atypical antipsychotic developed for the treatment of schizophrenia and acute mania associated with bipolar disorder by Schering-Plough after its November 19, 2007 merger with Organon International. Development of the drug, through Phase III trials, began while Organon was still... Clomipramine Clomipramine is a tricyclic antidepressant . It was developed in the 1960s by the Swiss drug manufacturer Geigy and has been in clinical use worldwide ever since.- Indications :... Clozapine Clozapine is an antipsychotic medication used in the treatment of schizophrenia, and is also used off-label in the treatment of bipolar disorder. Wyatt. R and Chew... EGIS-12233 EGIS-12,233 is a drug with applications in scientific research, acting as a potent and selective antagonist for both the 5-HT6 and 5-HT7 serotonin receptor subtypes, with good selectivity over other receptors. It has been shown to increase dopamine release in cochlear tissue, suggesting a role for... Iloperidone Iloperidone, also known as Fanapt, Fanapta, and previously known as Zomaril, is an atypical antipsychotic for the treatment of schizophrenia. It was approved by the U.S... MS-245 MS-245 is a tryptamine derivative which is used in scientific research. It acts as a selective 5-HT6 receptor antagonist with a Ki of 2.3 nM, and was derived through structure-activity relationship development of the selective 5-HT6 agonist EMDT. It has been used as a lead compound for further... Olanzapine Olanzapine is an atypical antipsychotic, approved by the FDA for the treatment of schizophrenia and bipolar disorder... Ro04-6790 Ro04-6790 is a drug, developed by Hoffmann–La Roche, which has applications in scientific research. It acts as a potent and selective receptor antagonist for the 5-HT6 serotonin receptor subtype, with little or no affinity at other receptors... SB-258,585 SB-258,585 is a drug which is used in scientific research. It acts as a potent, selective and orally active 5-HT6 receptor antagonist, with a Ki of 8.9nM... SB-271,046 SB-271,046 is a drug which is used in scientific research. It was one of the first selective 5-HT6 receptor antagonists to be discovered, and was found through high-throughput screening of the SmithKline Beecham Compound Bank using cloned 5-HT6 receptors as a target, with an initial lead compound... SB-357,134 SB-357,134 is a drug which is used in scientific research. It acts as a potent, selective and orally active 5-HT6 receptor antagonist. SB-357,134 and other 5-HT6 antagonists show nootropic effects in animal studies, and have been proposed as potential novel treatments for cognitive disorders such... SB-399,885 SB-399885 is a drug which is used in scientific research. It acts as a potent, selective and orally active 5-HT6 receptor antagonist, with a Ki of 9.0nM... |
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| 5-HT7 5-HT7 receptor The 5-HT7 receptor is a member of the GPCR superfamily of cell surface receptors and is activated by the neurotransmitter serotonin The 5-HT7 receptor is coupled to Gs and is expressed in a variety of human tissues, particularly in the brain, the gastrointestinal tract, and in various... |
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5-Carboxamidotryptamine 5-Carboxamidotryptamine is a tryptamine derivative closely related to the neurotransmitter serotonin.5-CT acts as a non-selective, high-affinity full agonist at the 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5A, and 5-HT7 receptors, as well as at the 5-HT2, 5-HT3, 5-HT6 receptors with lower affinity. It has... 8-OH-DPAT 8-OH-DPAT is a research chemical of the aminotetralin chemical class which was developed in the 1980s and has been widely used to study the function of the 5-HT1A receptor... AS-19 (drug) AS-19 is a substance which acts as a potent agonist at the 5HT7 receptor, with an IC50 of 0.83nM. It reverses the amnesia induced by drugs such as scopolamine and dizocilpine and improves long term memory acquisition, but inhibits short term memory formation.... |
Amitriptyline Amitriptyline is a tricyclic antidepressant . It is the most widely used TCA and has at least equal efficacy against depression as the newer class of SSRIs... Aripiprazole Aripiprazole is an atypical antipsychotic and antidepressant used in the treatment of schizophrenia, bipolar disorder, and clinical depression... Asenapine Asenapine is a new atypical antipsychotic developed for the treatment of schizophrenia and acute mania associated with bipolar disorder by Schering-Plough after its November 19, 2007 merger with Organon International. Development of the drug, through Phase III trials, began while Organon was still... Clomipramine Clomipramine is a tricyclic antidepressant . It was developed in the 1960s by the Swiss drug manufacturer Geigy and has been in clinical use worldwide ever since.- Indications :... Clozapine Clozapine is an antipsychotic medication used in the treatment of schizophrenia, and is also used off-label in the treatment of bipolar disorder. Wyatt. R and Chew... EGIS-12233 EGIS-12,233 is a drug with applications in scientific research, acting as a potent and selective antagonist for both the 5-HT6 and 5-HT7 serotonin receptor subtypes, with good selectivity over other receptors. It has been shown to increase dopamine release in cochlear tissue, suggesting a role for... Iloperidone Iloperidone, also known as Fanapt, Fanapta, and previously known as Zomaril, is an atypical antipsychotic for the treatment of schizophrenia. It was approved by the U.S... Imipramine Imipramine , also known as melipramine, is an antidepressant medication, a tricyclic antidepressant of the dibenzazepine group... Ketanserin Ketanserin is a drug with affinity for multiple G protein-coupled receptors . Initially it was believed to be a highly selective antagonist for serotonin 5-HT2A receptors, however this is not true. Ketanserin only has moderate selectivity for 5-HT2A receptors over 5-HT2C receptors... Mirtazapine Mirtazapine is a tetracyclic antidepressant used primarily in the treatment of depression. It is also sometimes used as a hypnotic, antiemetic, and appetite stimulant, and for the treatment of anxiety, among other indications... Olanzapine Olanzapine is an atypical antipsychotic, approved by the FDA for the treatment of schizophrenia and bipolar disorder... Ritanserin Ritanserin is a serotonin antagonist with possibilities for the treatment of many neurological disorders.When used together with typical antipsychotics in the treatment of schizophrenia is able to decrease negative symptoms and adds some "atypicality" as parkinsonism is slightly decreased.-... Risperidone Risperidone is a second generation or atypical antipsychotic, sold under the trade name . It is used to treat schizophrenia , schizoaffective disorder, the mixed and manic states associated with bipolar disorder, and irritability in people with autism... SB-269,970 SB-269,970 is a drug and research chemical developed by GlaxoSmithKline used in scientific studies. It was previously believed to act as a selective 5-HT7 receptor antagonist , but a subsequent discovery showed that it also potently blocks the α2-adrenergic receptor... |
Note that there is no 5-HT1C receptor since, after the receptor was cloned and further characterized, it was found to have more in common with the 5-HT2 family of receptors and was redesignated as the 5-HT2C receptor. Note that there is also no 5-HT5B receptor
5-HT5B receptor
5-HT5B receptor is a 5-HT receptor protein and the gene which encodes it. The protein is found in rodents, but not in humans, because stop codons in the gene's coding sequence prevent the gene from expressing a functional protein. It is believed that the function of the 5-HT5B receptor has been...
, as it exists only in mice and rats and not in humans or monkeys.
Very nonselective agonists of 5-HT receptor subtypes include ergotamine (an antimigraine
Antimigraine
An antimigraine drug is a medication intended to reduce the effects or intensity of migraine headache.Examples are the triptans, including zolmitriptan....
), which activates 5-HT1A, 5-HT1D, 5-HT1B, D2 and norepinephrine receptors. LSD (a psychedelic
Psychedelic
The term psychedelic is derived from the Greek words ψυχή and δηλοῦν , translating to "soul-manifesting". A psychedelic experience is characterized by the striking perception of aspects of one's mind previously unknown, or by the creative exuberance of the mind liberated from its ostensibly...
) is a 5-HT1A, 5-HT2A, 5-HT2C, 5-HT5A, 5-HT5, 5-HT6 agonist.