|5-hydroxytryptamine (serotonin) receptor 1B, G protein-coupled|
|Symbols||; 5-HT1B; 5-HT1DB; HTR1D2; HTR1DB; S12|
|External IDs||IUPHAR: ChEMBL: GeneCards:|
|RNA expression pattern|
Tissue distribution and function
5-HT1B receptors are widely distributed throughout the CNS with the highest concentrations found in the frontal cortex, basal ganglia, striatum, and the hippocampus. The function of the 5-HT1B receptor differs depending upon its location. In the frontal cortex, it is believed to act as a postsynaptic receptor inhibiting the release of dopamine. In the basal ganglia and the striatum, evidence suggests 5-HT signaling acts on an autoreceptor, inducing the release of serotonin and decreasing glutamatergic transmission by reducing miniature excitatory postsynaptic potential (mEPSP) frequency, respectively. In the hippocampus, a recent study has demonstrated that activation of postsynaptic 5-HT1B heteroreceptors produces a facilitation in excitatory synaptic transmission which is altered in depression. When the expression of 5-HT1B in human cortex is traced throughout life, A significant changes during adolescence was observed, in a way that is strongly correlated with the expression of 5-HT1E.
Outside the brain, 5-HT1B receptor activation also has vascular effects, such as pulmonary vasoconstriction. Furthermore, blocking 5-HT1B receptor signaling decreases the number of osteoblasts, bone mass, and the bone formation rate.
Knockout mice lacking the 5-HT1B gene have shown an increase in aggression and a higher preference for alcohol. Under basal conditions, knockout mice present with a "normal" phenotype and an exhibit a sucrose preference (lack of sucrose preference is considered a measure of anhedonia). However, after undergoing chronic unpredictable stress treatment to induce a "depression-like" phenotype these animals do not benefit from administration of selective serotonin reuptake inhibitor (SSRIs).
- ergotamine (vasoconstrictor in migraine)
- sumatriptan (vasoconstrictor in migraine)
- CP-93,129 (peripherally acting)
- CP-135,807 (mixed 5-HT1B/1D agonist)
- RU-24969 (mixed 5-HT1A/1B agonist)
Antagonists and inverse agonists
- methiothepin (antipsychotic)
- yohimbine (aphrodisiac)
- SB-224,289 (inverse agonist)
- SB-236,057 (inverse agonist)
In humans the protein is coded by the gene HTR1B.
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