5-HT1B receptor
Encyclopedia
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.
.
Blocking the 5-HT1B receptor decreases the number of osteoblast
s, bone mass, and the bone formation rate.
5-HT1B receptors are present in many parts of the human brain. The highest concentrations are found in the basal ganglia
, striatum
and the frontal cortex.
The function of the receptor differs between the areas: in the frontal cortex it is believed to act as a terminal receptor, inhibiting the release of dopamine
. In the striatum and the basal ganglia, the 5-HT1B receptor is thought to act as an autoreceptor, inhibiting the release of serotonin
.
Knockout mice lacking the 5-HT1B gene have shown an increase of aggression and a higher preference for alcohol.
A genetic variant in the promotor region, A-161T, has been examined with respect to personality traits and showed no major effect.
Protein
Proteins are biochemical compounds consisting of one or more polypeptides typically folded into a globular or fibrous form, facilitating a biological function. A polypeptide is a single linear polymer chain of amino acids bonded together by peptide bonds between the carboxyl and amino groups of...
that in humans is encoded by the HTR1B gene
Gene
A gene is a molecular unit of heredity of a living organism. It is a name given to some stretches of DNA and RNA that code for a type of protein or for an RNA chain that has a function in the organism. Living beings depend on genes, as they specify all proteins and functional RNA chains...
. The 5-HT1B receptor is a 5-HT receptor
5-HT receptor
The serotonin receptors, also known as 5-hydroxytryptamine receptors or 5-HT receptors, are a group of G protein-coupled receptors and ligand-gated ion channels found in the central and peripheral nervous systems. They mediate both excitatory and inhibitory neurotransmission...
subtype.
Tissue distribution and function
The 5-HT1B receptor acts on the CNS, where it induces presynaptic inhibition and behavioural effects. It also has vascular effects, such as pulmonary vasoconstrictionVasoconstriction
Vasoconstriction is the narrowing of the blood vessels resulting from contraction of the muscular wall of the vessels, particularly the large arteries, small arterioles and veins. The process is the opposite of vasodilation, the widening of blood vessels. The process is particularly important in...
.
Blocking the 5-HT1B receptor decreases the number of osteoblast
Osteoblast
Osteoblasts are mononucleate cells that are responsible for bone formation; in essence, osteoblasts are specialized fibroblasts that in addition to fibroblastic products, express bone sialoprotein and osteocalcin.Osteoblasts produce a matrix of osteoid, which is composed mainly of Type I collagen...
s, bone mass, and the bone formation rate.
5-HT1B receptors are present in many parts of the human brain. The highest concentrations are found in the basal ganglia
Basal ganglia
The basal ganglia are a group of nuclei of varied origin in the brains of vertebrates that act as a cohesive functional unit. They are situated at the base of the forebrain and are strongly connected with the cerebral cortex, thalamus and other brain areas...
, striatum
Striatum
The striatum, also known as the neostriatum or striate nucleus, is a subcortical part of the forebrain. It is the major input station of the basal ganglia system. The striatum, in turn, gets input from the cerebral cortex...
and the frontal cortex.
The function of the receptor differs between the areas: in the frontal cortex it is believed to act as a terminal receptor, inhibiting the release of 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...
. In the striatum and the basal ganglia, the 5-HT1B receptor is thought to act as an autoreceptor, inhibiting the release of 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...
.
Knockout mice lacking the 5-HT1B gene have shown an increase of aggression and a higher preference for alcohol.
Agonists
- ergotamine (vasoconstrictor in migraine)
- sumatriptanSumatriptanSumatriptan is a triptan sulfa drug containing a sulfonamide group. It is used for the treatment of migraine headaches. Sumatriptan is produced and marketed by various drug manufacturers with many different trade names such as Sumatriptan, Imitrex, Imigran, Imigran recovery.-Approval and...
(vasoconstrictor in migraine) - zolmitriptanZolmitriptanZolmitriptan is a selective serotonin receptor agonist of the 1B and 1D subtypes. It is a triptan, used in the acute treatment of migraine attacks with or without aura and cluster headaches....
- 5-Carboxamidotryptamine5-Carboxamidotryptamine5-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...
- CGS-12066ACGS-12066ACGS-12066A is a drug which acts as a potent and selective agonist for the 5-HT1B receptor with lower affinity for the three 5-HT2 receptor subtypes. It is used for studying the role of the 5-HT1B receptor in various processes including perception of pain and the sleep-wake cycle.-References:...
- CP-93,129 (peripherally acting)
- CP-94,253CP-94,253CP-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...
- CP-135,807 (mixed 5-HT1B/1D agonist)
- RU-24969 (mixed 5-HT1A/1B agonist)
Antagonists and inverse agonists
- methiothepin (antipsychoticAntipsychoticAn 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...
) - yohimbineYohimbineYohimbine 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...
(aphrodisiacAphrodisiacAn aphrodisiac is a substance that increases sexual desire. The name comes from Aphrodite, the Greek goddess of sexuality and love. Throughout history, many foods, drinks, and behaviors have had a reputation for making sex more attainable and/or pleasurable...
) - metergolineMetergolineMetergoline is a psychoactive drug of the ergoline chemical class which acts as a ligand for various serotonin and dopamine receptors....
- isamoltaneIsamoltaneIsamoltane 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....
- AR-A000002AR-A000002AR-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...
- SB-216,641SB-216,641SB-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....
- SB-224,289 (inverse agonist)
- SB-236,057 (inverse agonist)
Genetics
In humans the protein is coded by the gene HTR1B.A genetic variant in the promotor region, A-161T, has been examined with respect to personality traits and showed no major effect.