5-HT receptor

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5-HT receptor

In the field of neurochemistry

Neurochemistry

Neurochemistry is the specific study of neurochemicals, which include neurotransmitters and other molecules such as neuro-active drugs that influence neuron function....
, 5-HT receptors are receptors

Receptor (biochemistry)

In biochemistry, a receptor is a protein molecule, embedded in either the plasma membrane or cytoplasm of a cell, to which a mobile signaling molecule may attach....
for the neurotransmitter

Neurotransmitter

Neurotransmitters are chemistry which relay, amplify and modulate signals between a neuron and another cell . Neurotransmitters are packaged into vesicles that cluster beneath the membrane on the presynaptic side of a synapse, and are released into the synaptic cleft, where they bind to receptors in the membrane on the postsynaptic side of...
and peripheral

Periphery

Generally, a periphery is a boundary or outer part of any space or body....
signal mediator serotonin

Serotonin

Serotonin is a monoamine neurotransmitter synthesized in serotonergic neurons in the central nervous system and enterochromaffin cells in the gastrointestinal tract of animals including humans....
, also known as 5-hydroxytryptamine or 5-HT. 5-HT receptors are located on the cell membrane of nerve cells

Neuron

Neurons are responsive cell in the nervous system that process and transmit information by electrochemical Signal . They are the core components of the brain, the vertebrate spinal cord, the invertebrate ventral nerve cord, and the peripheral nerves....
and other cell types including smooth muscle in animals, and mediate the effects of serotonin as the endogenous

Endogenous

The word endogenous means "arising from within", the opposite of exogenous....
ligand

Ligand

In chemistry, a ligand is either an atom, ion, or molecule that bonds to a central metal, generally involving formal donation of one or more of its electrons....
and of a broad range of pharmaceutical and hallucinogenic drugs

Psychedelics, dissociatives and deliriants

The general group of pharmacology agents commonly known as hallucinogens can be divided into three broad categories: Psychedelic drugs, dissociatives, and deliriants....
. 5-HT receptors affect the release and activity of other neurotransmitters such as glutamate, dopamine

Dopamine

Dopamine is a neurotransmitter occurring in a wide variety of animals, including both vertebrates and invertebrates. In the human brain, this phenethylamine functions as a neurotransmitter, activating the five types of dopamine receptors ? D1, D2, D3, D4 and D5, and their variants....
and GABA

Gabâ

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Encyclopedia

In the field of neurochemistry

Neurochemistry

Receptor (biochemistry)

In biochemistry, a receptor is a protein molecule, embedded in either the plasma membrane or cytoplasm of a cell, to which a mobile signaling molecule may attach....
for the neurotransmitter

Neurotransmitter

Periphery

Generally, a periphery is a boundary or outer part of any space or body....
signal mediator serotonin

Serotonin

Neuron

Endogenous

The word endogenous means "arising from within", the opposite of exogenous....
ligand

Ligand

Psychedelics, dissociatives and deliriants

Dopamine

Gabâ

Gab? or gabaa, for the Cebuano people , is the concept of a non-human and non-divine, imminent Retributive justice. A sort of negative karma, it is generally seen as an evil effect on a person because of their wrongdoings or transgressions....
. 5-HT_2A receptors increase the activity of glutamate in many areas of the brain, while some other serotonin receptors have the effect of suppressing glutamate. Increased stimulation of 5-HT_2A receptors seem to oppose the therapeutic actions of increased stimulation of other serotonin receptors in anti-depressant and anxiolytic

Anxiolytic

An anxiolytic is a Medication prescribed for the treatment of symptoms of anxiety. Some anxiolytics have been shown to be useful in the treatment of anxiety disorders as have antidepressants such as the class of selective serotonin reuptake inhibitors ....
treatments.

Classification

With the exception of the 5-HT₃ receptor

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 Gamma-aminobutyric acid and glycine receptor....
, a ligand gated ion channel, all other 5-HT receptors are G protein coupled seven transmembrane (or heptahelical) receptors 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 "....
second messenger cascade.

Families

Family	Type	Mechanism >- \| 5-HT₁	G_i/G_o Gi alpha subunit Gi alpha subunit is a heterotrimeric G protein subunit which inhibits the production of Cyclic_adenosine_monophosphate from Adenosine triphosphate.... coupled	decreasing cellular levels of cAMP Cyclic adenosine monophosphate Cyclic adenosine monophosphate is a second messenger that is important in many biological processes. cAMP is derived from adenosine triphosphate and used for intracellular signal transduction in many different organisms.... \|- \| 5-HT₂	G_q/G₁₁ coupled	increasing cellular levels of inositol trisphosphate (IP₃) and diacylglycerol Diglyceride A diglyceride, or a diacylglycerol , is a glyceride consisting of two fatty acid chains covalent bond to a glycerol molecule through ester linkages.... (DAG) \|- \| 5-HT₃	ligand-gated Na⁺ Sodium Sodium is an element which has the symbol Na , atomic number 11, atomic mass 23 amu , and a common oxidation number +1. Sodium is a soft, silvery white, highly reactive element and is a member of the alkali metals within "group 1" .... and K⁺ Potassium Potassium is a chemical element. It has the symbol K , atomic number 19, and atomic mass 39.0983. Potassium was first isolated from potash, hence the name.... cation channel	depolarizing Depolarization In biology, depolarization is a decrease in the absolute value of a cell's membrane potential. Thus, changes in membrane voltage in which the membrane potential becomes less positive or less negative are both depolarizations.... plasma membrane \|- \| 5-HT₄	G_s coupled	- \| 5-HT_5A	G protein G protein G proteins, short for guanine nucleotide-binding proteins, are a family of proteins involved in second messenger cascades.G proteins are so called because they function as "molecular switches," alternating between an inactive guanosine diphosphate and active guanosine triphosphate bound state, ultimately going on to regulate down... coupled; the primary coupling appears to be through Gi/o	inhibiting adenylate cyclase Adenylate cyclase Adenylate cyclase is a lyase enzyme.... activity.
5-HT₆	G_s coupled	- \| 5-HT₇	G_s coupled	increasing cellular levels of cAMP

Specific proteins/genes

Within these general classes of 5-HT receptors, a number of specific types have been characterized:

Receptor	Actions	Agonist Agonist An agonist is a term used to describe a type of Ligand or drug that binds and alters the activity of a Receptor . The ability to alter the activity of a receptor, also known as the agonist's efficacy is a property that distinguishes it from receptor antagonist, a type of receptor ligand which also binds a receptor but which does not alter t... 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
Summary of characterized 5-HT receptors with selected high affinity agonist and antagonist ligands Ligand (biochemistry) In biochemistry, a ligand is a Chemical substance that is able to bind to and form a Complex with a biomolecule to serve a biological purpose.... , both ones of major importance and others
5-HT_1A 5-HT1A receptor 5-hydroxytryptamine receptor 1A is a 5-HT1 receptor.HTR1A denotes the human gene encoding it.5-HT1A acts on the central nervous system, where it controls functions such as sleep, feeding, thermoregulation, mood, aggression, and anxiety....	CNS Central nervous system The central nervous system is the part of the nervous system that functions to coordinate the activity of all parts of the bodies of multicellular organisms.... : neuronal inhibition, behavioural effects (sleep, feeding, thermoregulation Thermoregulation Thermoregulation is the ability of an organism to keep its core temperature within certain boundaries, even when the surrounding temperature is very different.... , aggression, anxiety)	buspirone Buspirone Buspirone is an anxiolytic agent and a serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the benzodiazepines, but it has an efficacy comparable to diazepam in treating generalized anxiety disorder.... LSD LSD Lysergic acid diethylamide, LSD, LSD-25, or acid, is a semisynthetic psychedelic drug of the ergoline family. Its unusual psychological effects, which include visuals of colored patterns behind the eyes in the mind, a sense of time distorting, and crawling geometric patterns, have made it one of the most widely known psyched... psilocin Psilocin Psilocin sometimes also spelled psilocine, psilocyn, or psilotsin, is a psychedelic drug mushroom alkaloid. It is found in most psychedelic mushrooms together with its phosphorylated counterpart psilocybin.... MDMA Methylenedioxymethamphetamine MDMA , most commonly known today by the street name ecstasy , is a semisynthetic member of the amphetamine class of psychoactive drugs, a subclass of the phenethylamines..... (speculated) 5-CT 5-Carboxamidotryptamine 5-Carboxamidotryptamine is a drug which acts as a non-selective agonist at several different serotonin Receptor . It was initially thought to be selective for 5HT1, but subsequent research showed that it also acts at 5HT2, 5HT3, 5HT5 and 5HT7, although its strongest effect is at the 5HT<... 8-OH-DPAT 8-OH-DPAT 8-OH-DPAT is a substance which acts as an agonist of the 5-HT1A receptor and 5-HT7 receptor Receptor s. It can elicit pelvic floor contractions.... flesinoxan Flesinoxan Flesinoxan is an anxiolytic drug which acts as a selective 5-HT1A receptor agonist.References ... U-92016A vilazodone Vilazodone Vilazodone is a dual-mechanism antidepressant and anxiolytic drug. It functions as both an SSRI, and a 5-HT1A receptor agonist. Vilazodone is currently in phase III clinical trials....	ergotamine Ergotamine Ergotamine is an ergopeptine and part of the ergot family of alkaloids; it is structurally and biochemically closely related to ergoline. It possesses structural similarity to several neurotransmitters, and has biological activity as a vasoconstrictor.... pindolol Pindolol Pindolol is a beta blocker drug.... yohimbine Yohimbine Yohimbine, also known under the antiquated names quebrachin, aphrodin, corynine, yohimvetol, and hydroergotocin, is a purported aphrodisiac.... methiothepin robalzotan spiperone Spiperone Spiperone is an antipsychotic drug which is a butyrophenone derivative .It acts on subsets of both 5-HT receptors and dopamine receptors, and is used to treat schizophrenia.... WAY-100135 WAY-100635 WAY-100635 WAY-100,635 is an agent that is a Efficacy#Pharmacology human dopamine receptor D4 full agonist,and a receptor antagonist for the 5-HT1A receptor....
5-HT_1B 5-HT1B receptor 5-hydroxytryptamine receptor 1B, also known as HTR1B, is a human 5-HT receptor, but also denotes the gene encoding it....	CNS: presynaptic inhibition, behavioural effects vascular: pulmonary vasoconstriction Vasoconstriction Vasoconstriction is the narrowing of the blood vessels resulting from contraction of the muscular wall of the vessels, particularly the large arteries, arterioles and veins....	ergotamine Ergotamine Ergotamine is an ergopeptine and part of the ergot family of alkaloids; it is structurally and biochemically closely related to ergoline. It possesses structural similarity to several neurotransmitters, and has biological activity as a vasoconstrictor.... sumatriptan Sumatriptan Sumatriptan is a triptan drug including a sulfonamide group for the treatment of migraine headaches. It is marketed and manufactured by GlaxoSmithKline....	risperidone Risperidone Risperidone is an atypical antipsychotic developed by Janssen-Cilag.... yohimbine Yohimbine Yohimbine, also known under the antiquated names quebrachin, aphrodin, corynine, yohimvetol, and hydroergotocin, is a purported aphrodisiac.... metergoline Metergoline Metergoline is a synthetic compound, that acts on subsets of both 5-HT receptors and dopamine receptors. Metergoline has been reported to be a 5-HT1D receptor receptor agonist.... methiothepin
5-HT_1D 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....	CNS: locomotion, anxiety; vascular: cerebral vasoconstriction Vasoconstriction Vasoconstriction is the narrowing of the blood vessels resulting from contraction of the muscular wall of the vessels, particularly the large arteries, arterioles and veins....	sumatriptan Sumatriptan Sumatriptan is a triptan drug including a sulfonamide group for the treatment of migraine headaches. It is marketed and manufactured by GlaxoSmithKline.... 5-(Nonyloxy)tryptamine	ergotamine Ergotamine Ergotamine is an ergopeptine and part of the ergot family of alkaloids; it is structurally and biochemically closely related to ergoline. It possesses structural similarity to several neurotransmitters, and has biological activity as a vasoconstrictor.... yohimbine Yohimbine Yohimbine, also known under the antiquated names quebrachin, aphrodin, corynine, yohimvetol, and hydroergotocin, is a purported aphrodisiac.... metergoline Metergoline Metergoline is a synthetic compound, that acts on subsets of both 5-HT receptors and dopamine receptors. Metergoline has been reported to be a 5-HT1D receptor receptor agonist.... methiothepin
5-HT_1E		BRL-54443 LSD LSD Lysergic acid diethylamide, LSD, LSD-25, or acid, is a semisynthetic psychedelic drug of the ergoline family. Its unusual psychological effects, which include visuals of colored patterns behind the eyes in the mind, a sense of time distorting, and crawling geometric patterns, have made it one of the most widely known psyched... (very low)
5-HT_1F		BRL-54443 LY-334,370 LY-344,864
5-HT_2A 5-HT2A receptor The mammalian 5-HT2A receptor is a subtype of the 5-HT2 receptor which belongs to the serotonin receptor family and is a GPCR ....	CNS: neuronal excitation, behavioural effects, learning, anxiety smooth muscle: contraction, vasoconstriction Vasoconstriction Vasoconstriction is the narrowing of the blood vessels resulting from contraction of the muscular wall of the vessels, particularly the large arteries, arterioles and veins.... / vasodilatation platelets: aggregation	mescaline Mescaline Mescaline or 3,4,5-trimethoxyphenethylamine is a naturally-occurring psychedelic alkaloid of the phenethylamine class. It is mainly used as a recreational drug, an entheogen, and a tool to supplement various practices for transcendence , including in meditation, psychonautics, art projects, and psychedelic psychotherapy.... psilocin Psilocin Psilocin sometimes also spelled psilocine, psilocyn, or psilotsin, is a psychedelic drug mushroom alkaloid. It is found in most psychedelic mushrooms together with its phosphorylated counterpart psilocybin.... DOI 2,5-Dimethoxy-4-iodoamphetamine DOI or 2,5-dimethoxy-4-iodoamphetamine is a psychedelic drug and a substituted amphetamine of the phenethylamine family. Despite being a Substitution amphetamine it is not a stimulant.... a-methyl-5-HT 5-MeO-AMT 5-MeO-AMT 5-MeO-AMT or 5-methoxy-a-methyltryptamine is a potent Psychedelics, dissociatives and deliriants tryptamines. It is soluble in alcohol.... DMT DMT DMT is a three-letter abbreviation which may stand for* Dimethyltryptamine, a hallucinogenic tryptamine* Dance Movement Therapy* Dimethyl terephthalate... LSD LSD Lysergic acid diethylamide, LSD, LSD-25, or acid, is a semisynthetic psychedelic drug of the ergoline family. Its unusual psychological effects, which include visuals of colored patterns behind the eyes in the mind, a sense of time distorting, and crawling geometric patterns, have made it one of the most widely known psyched... “Bromo-DragonFLY Bromo-DragonFLY Bromo-DragonFLY, also known as ABDF, or "Placid" is a psychedelic Psychedelics, dissociatives and deliriants related to the phenethylamine family.... ” TCB-2 TCB-2 TCB-2 is a conformationally restricted derivative of the phenethylamine derived hallucinogen 2C-B, discovered in 2006 by a team at Purdue University.... 25I-NBOMe 25I-NBOMe 25I-NBOMe is a derivative of the phenethylamine psychedelic 2C-I, discovered in 2006 by a team at Purdue University. It acts as a potent agonist for the 5HT2A receptor Receptor with a Dissociation constant of 0.087nM at the human 5HT2A receptor, making it some seven times the potency of 2C-I itself....	ketanserin Ketanserin Ketanserin is a serotonin antagonist.It has the highest affinity for the serotonin 5-HT2A receptor, but also Binding less potently to the 5-HT2C receptor, 5-HT2B receptor, 5-HT1D receptor, Adrenergic receptor, and dopamine receptors.... mirtazapine Mirtazapine Mirtazapine is an antidepressant introduced by Organon International in 1994 used for the treatment of moderate to severe clinical depression.... nefazodone Nefazodone Nefazodone hydrochloride is an antidepressant drug marketed by Bristol-Myers Squibb. Its sale was discontinued in 2003 in some countries, due to the small possibility of hepatic injury, which could lead to the need for a liver transplant, or even death.... pizotifen Pizotifen Pizotifen or pizotyline , trade name Sandomigran, is a benzocycloheptane based drug used as a medicine, primarily as a preventative to reduce the frequency of recurrent migraine headaches.... trazodone Trazodone Trazodone is a psychoactive compound with sedative, anxiolytic, and antidepressant properties. The various manufacturers claim that the antidepressant becomes active in the first week of therapy.... atypical antipsychotics cyproheptadine Cyproheptadine Cyproheptadine is an antihistamine/anticholinergic and antiserotonergic agent. It acts as a 5-HT receptor receptor antagonist and also blocks calcium channels....
5-HT_2B 5-HT2B receptor 5-hydroxytryptamine receptor 2B, also known as HTR2B, is a 5-HT2 receptor, but also denotes the human gene encoding it....	stomach: contraction	LSD LSD Lysergic acid diethylamide, LSD, LSD-25, or acid, is a semisynthetic psychedelic drug of the ergoline family. Its unusual psychological effects, which include visuals of colored patterns behind the eyes in the mind, a sense of time distorting, and crawling geometric patterns, have made it one of the most widely known psyched... BW-723C86 BW-723C86 BW-723C86 is a tryptamine derivative drug which acts as a selective 5-HT2B receptor 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 Fenfluramine is a drug that was part of the Fen-Phen anti-obesity medication . Also known as Pondimin, fenfluramine was introduced on the U.S.... a-methyl-5-HT DOI 2,5-Dimethoxy-4-iodoamphetamine DOI or 2,5-dimethoxy-4-iodoamphetamine is a psychedelic drug and a substituted amphetamine of the phenethylamine family. Despite being a Substitution amphetamine it is not a stimulant.... MDMA	yohimbine Yohimbine Yohimbine, also known under the antiquated names quebrachin, aphrodin, corynine, yohimvetol, and hydroergotocin, is a purported aphrodisiac.... RS-127,445 RS-127,445 RS-127,445 is a drug which acts as a potent and selective Antagonist at the serotonin 5-HT2B receptor Receptor , with around 1000x selectivity over the closely related 5-HT2A receptor and 5-HT2C receptor receptors.... SB-204,741 SB-204,741 SB-204,741 is a drug which acts as a potent and selective Antagonist at the serotonin 5-HT2B receptor Receptor , with around 135x selectivity over the closely related 5-HT2C receptor receptor, and even higher over the 5-HT2A receptor receptor and other targets.... LY-272,015 LY-272,015 LY-272,015 is a beta-carboline derivative drug developed by Eli Lilly and Company, which acts as a potent and selective Antagonist at the serotonin 5-HT2B receptor Receptor ....
5-HT_2C 5-HT2C receptor 5-hydroxytryptamine receptor 2C, also known as HTR2C, is a 5-HT2 receptor, but also denotes the human gene encoding it....	CNS: anxiety, choroid plexus Choroid plexus The choroid plexus is the area on the ventricle s of the brain where cerebrospinal fluid is produced by modified ependymal cells.... : cerebrospinal fluid Cerebrospinal fluid Cerebrospinal fluid , Liquor cerebrospinalis, is a clear bodily fluid that occupies the subarachnoid space and the ventricular system around and inside the brain.... (CSF) secretion	Lorcaserin Lorcaserin Lorcaserin is a serotonergic weight-loss drug developed by Arena Pharmaceuticals. It is currently undergoing the final phase of clinical trials in preparation for submission for FDA approval.... LSD LSD Lysergic acid diethylamide, LSD, LSD-25, or acid, is a semisynthetic psychedelic drug of the ergoline family. Its unusual psychological effects, which include visuals of colored patterns behind the eyes in the mind, a sense of time distorting, and crawling geometric patterns, have made it one of the most widely known psyched... psilocin Psilocin Psilocin sometimes also spelled psilocine, psilocyn, or psilotsin, is a psychedelic drug mushroom alkaloid. It is found in most psychedelic mushrooms together with its phosphorylated counterpart psilocybin.... a-methyl-5-HT DOI 2,5-Dimethoxy-4-iodoamphetamine DOI or 2,5-dimethoxy-4-iodoamphetamine is a psychedelic drug and a substituted amphetamine of the phenethylamine family. Despite being a Substitution amphetamine it is not a stimulant.... A-372,159 A-372,159 A-372,159 is a drug which acts as a potent and selective partial agonist for the 5HT2C receptor Receptor , with more than 100x selectivity over the closely related 5-HT2B receptor receptor and a Dissociation constant of 3nM.... YM-348 YM-348 YM-348 is an indazole derivative drug which acts as a potent and selective 5-HT2C receptor Receptor agonist, with an EC50 of 1nM and 15x selectivity over 5-HT2A receptor, although it only has moderate selectivity of 3x over the closely related 5-HT2B receptor receptor....	fluoxetine Fluoxetine Fluoxetine hydrochloride is an antidepressant of the selective serotonin reuptake inhibitor class. Fluoxetine is approved for the treatment of major depressive disorder , obsessive-compulsive disorder , bulimia nervosa, anorexia nervosa, panic disorder and premenstrual dysphoric disorder.... methysergide Methysergide Methysergide is a prescription drug used for prophylaxis of migraine and is sold under the brand names Sansert and Deseril in 2mg dosages.... agomelatine Agomelatine Agomelatine is a chemical compound that is structurally closely related to melatonin. Agomelatine is a potent agonist at melatonin receptors and an Receptor antagonist at serotonin-2C receptors,... mesulergine Mesulergine Mesulergine is a synthetic compound, that acts on subsets of both 5-HT receptors and dopamine receptors.The compound had entered clinical trials for the treatment of Parkinson's disease, however further development was halted due to adverse histology abnormalities in rats.... RS-102,221 RS-102,221 RS-102,221 is a drug developed by Hoffmann?La Roche, which was one of the first compounds discovered that acts as a potent and selective Antagonist at the serotonin 5-HT2C receptor Receptor , with around 100x selectivity over the closely related 5-HT2A receptor and 5-HT2B receptor receptors.... SB-242,084 SB-242,084 SB-242,084 is a drug which acts as a selective Receptor antagonist for the 5HT2C receptor Receptor . It has anxiolytic effects, and enhances dopamine signalling in the limbic system, as well as having complex effects on the dopamine release produced by cocaine, increasing it in some brain regions but reducing it in others....
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 Gamma-aminobutyric acid and glycine receptor....	CNS, PNS Peripheral nervous system The peripheral nervous system resides or extends outside the central nervous system , which consists of the brain and spinal cord. The main function of the PNS is to connect the CNS to the limbs and organs.... : neuronal excitation, anxiety, emesis	2-methyl-5-HT Quipazine Quipazine Quipazine is a piperazine-based serotonin Receptor agonist. It is moderately selective, binding to a range of different serotonin receptors, but particularly to the 5-HT2A receptor and 5-HT3 receptor receptors.... RS-56812 RS-56812 RS-56812 is a potent and selective partial agonist for the ligand-gated ion channel serotonin Receptor 5-HT3 receptor. It has been shown to improve performance on animal tests of memory....	alosetron Alosetron Alosetron is a 5-HT3 antagonist used for the management of severe diarrhoea-predominant irritable bowel syndrome in women only. It is currently marketed by Prometheus Laboratories Inc.... memantine Memantine Memantine is the first in a novel class of Alzheimer's disease medications acting on the glutamatergic system by blocking NMDA glutamate receptors.... metoclopramide Metoclopramide Metoclopramide is a potent dopamine receptor antagonist used for its antiemetic and prokinetic properties. Thus it is primarily used to treat nausea and vomiting, and to facilitate gastric emptying in patients with gastroparesis.... (high doses) mirtazapine Mirtazapine Mirtazapine is an antidepressant introduced by Organon International in 1994 used for the treatment of moderate to severe clinical depression.... ondansetron Ondansetron Ondansetron or GlaxoSmithKline's Zofran is a serotonin 5-HT3 antagonist used mainly as an antiemetic to treat nausea and vomiting following chemotherapy.... renzapride Renzapride Renzapride is a full serotonin 5-HT4 receptor agonist, partial serotonin 5-HT3 and 5-HT2b receptor antagonist....
5-HT₄ 5-HT4 receptor 5-hydroxytryptamine receptor 4, also known as HTR4, is a human gene....	GIT Gastrointestinal tract The digestive tract is the system of Organ s within multicellular animals that takes in food, digestion it to extract energy and nutrients, and expels the remaining waste.... : gastrointestinal motility CNS: neuronal excitation, learning, memory	cisapride Cisapride Cisapride is a parasympathomimetic which acts as a serotonin 5-HT4 receptor agonist. Stimulation of the serotonin receptors increases acetylcholine release in the enteric nervous system.... metoclopramide Metoclopramide Metoclopramide is a potent dopamine receptor antagonist used for its antiemetic and prokinetic properties. Thus it is primarily used to treat nausea and vomiting, and to facilitate gastric emptying in patients with gastroparesis.... tegaserod Tegaserod Tegaserod is a serotonin4 agonist manufactured by Novartis and used for the management of irritable bowel syndrome and constipation. Its use was the only drug approved by the United States of America Food and Drug Administration to help relieve the abdomen discomfort, bloating and constipation associated with irritable bowel syndro... 5-MT 5-Methoxytryptamine 5-Methoxytryptamine, also known as mexamine or meksamin, is a methylated derivative of serotonin . It is also the acetyl derivative of melatonin.... renzapride Renzapride Renzapride is a full serotonin 5-HT4 receptor agonist, partial serotonin 5-HT3 and 5-HT2b receptor antagonist.... BIMU-8 RS 67333 RS 67333 RS-67333 is a 5-HT receptor partial agonist, being researched as a possible rapid acting antidepressant, nootropic, and treatment for Alzheimer's....	GR-113,808 Piboserod Piboserod Piboserod is a selective 5-HT4 receptor receptor antagonist which was marketed and manufactured by GlaxoSmithKline under the trade name Serlipet for the management of atrial_fibrillation and irritable_bowel_syndrome ....
5-HT_5A 5-HT5A receptor 5-hydroxytryptamine receptor 5A, also known as HTR5A, is a protein which in humans is encoded by the HTR5A gene....	CNS (cortex Cerebral cortex The cerebral cortex is a structure within the brain that plays a key role in memory, attention, perceptual awareness, thought, language, and consciousness.... , hippocampus Hippocampus The hippocampus is a brain structure located inside the medial temporal lobe of the cerebral cortex, and therefore is part of the telencephalon .... , cerebellum Cerebellum The cerebellum is a region of the brain that plays an important role in the integration of perception, coordination and motoneuron control. In order to coordinate motor control, there are many neural pathways linking the cerebellum with the cerebrum motor cortex and the spinocerebellar tract .... ): unknown	LSD LSD Lysergic acid diethylamide, LSD, LSD-25, or acid, is a semisynthetic psychedelic drug of the ergoline family. Its unusual psychological effects, which include visuals of colored patterns behind the eyes in the mind, a sense of time distorting, and crawling geometric patterns, have made it one of the most widely known psyched... 5-CT 5-Carboxamidotryptamine 5-Carboxamidotryptamine is a drug which acts as a non-selective agonist at several different serotonin Receptor . It was initially thought to be selective for 5HT1, but subsequent research showed that it also acts at 5HT2, 5HT3, 5HT5 and 5HT7, although its strongest effect is at the 5HT<...	SB-699,551-A
5-HT₆ 5-HT6 receptor The 5-HT6 receptor, also known as the 5-hydroxytryptamine receptor 6 , is a human gene. The 5-HT6 receptor is primarily expressed in the brain and is involved in glutamic acid and cholinergic neuron activity....	CNS: regulates glutamate and acetylcholine release	LSD LSD Lysergic acid diethylamide, LSD, LSD-25, or acid, is a semisynthetic psychedelic drug of the ergoline family. Its unusual psychological effects, which include visuals of colored patterns behind the eyes in the mind, a sense of time distorting, and crawling geometric patterns, have made it one of the most widely known psyched... EMDT 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 Receptor agonist, with a Dissociation constant of 16nM, and was one of the first selective agonists developed for this serotonin receptor subtype.... EMD-386,088 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 Receptor agonist, with a Dissociation constant of 1nM, a significantly higher affinity than older 5-HT6 agonists such as 2-Ethyl-5-methoxy-N,N-dimethyltryptamine, although it does also have moderate affinity f...	SB-271,046 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 Receptor Antagonist 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 being developed into SB-2... SB-258,585 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 Receptor Antagonist , with a Dissociation constant of 8.9nM.... SB-357,134 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 Receptor Antagonist .... SB-399,885 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 Receptor Antagonist , with a Dissociation constant of 9.0nM....
5-HT₇ 5-HT7 receptor 5-hydroxytryptamine receptor 7 , also known as HTR7, is protein which in humans is encoded by the HTR7 gene. The 5-HT7 receptor is activated by the neurotransmitter serotonin....	CNS, GIT, blood vessels: unknown	5-CT 5-Carboxamidotryptamine 5-Carboxamidotryptamine is a drug which acts as a non-selective agonist at several different serotonin Receptor . It was initially thought to be selective for 5HT1, but subsequent research showed that it also acts at 5HT2, 5HT3, 5HT5 and 5HT7, although its strongest effect is at the 5HT<... LSD LSD Lysergic acid diethylamide, LSD, LSD-25, or acid, is a semisynthetic psychedelic drug of the ergoline family. Its unusual psychological effects, which include visuals of colored patterns behind the eyes in the mind, a sense of time distorting, and crawling geometric patterns, have made it one of the most widely known psyched... AS-19 AS-19 (drug) AS-19 is a substance which acts as a potent agonist at the 5-HT7 receptor 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....	risperidone Risperidone Risperidone is an atypical antipsychotic developed by Janssen-Cilag.... methiothepin

Note that there is no 5-HT_1C 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-HT_2C receptor.

Therapeutic modulation

Various drugs

Medication

A pharmaceutical drug, also referred to as medicine or medicament, can be loosely defined as any substance intended for use in the diagnosis, cure, mitigation, treatment, or prevention of disease....
are used to modulate the 5-HT system including some antidepressant

Antidepressant

An antidepressant is a psychiatric medication used for alleviating major depressive disorder or dysthymia. Drug groups known as MAOIs, tricyclics, and second-generation antidepressants such as SSRIs, and serotonin-norepinephrine reuptake inhibitors are particularly associated with the term....
s, anxiolytic

Anxiolytic

Antiemetic

An antiemetic is a medication that is effective against vomiting and nausea. Anti-emetics are typically used to treat motion sickness and the Adverse effect of opioid analgesics, general anaesthetics and chemotherapy directed against cancer....
s, antipsychotics and anti-migraine agents

Triptan

Triptans are a family of tryptamine based medication used as abortive medication in the treatment of migraine and cluster headaches. They were first introduced in the 1990s....
.

5-HT receptor

Classification

Families

Specific proteins/genes

Therapeutic modulation

External links