Samiksha Jaiswal (Editor)

5 HT1B receptor

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Covid-19
Species  Human
Entrez  3351
Human  Mouse
Ensembl  ENSG00000135312
5-HT1B receptor
Aliases  HTR1B, 5-HT1B, 5-HT1DB, HTR1D2, HTR1DB, S12, 5-HT-1B, 5-HT-1D-beta, 5-hydroxytryptamine receptor 1B
External IDs  MGI: 96274 HomoloGene: 669 GeneCards: HTR1B

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.

Contents

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, inhibiting 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 was traced throughout life, significant changes during adolescence were 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 signalling increases 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 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).

Agonists

  • ergotamine (vasoconstrictor in migraine)
  • Oxymetazoline
  • sumatriptan (vasoconstrictor in migraine)
  • zolmitriptan
  • 5-Carboxamidotryptamine
  • CGS-12066A
  • CP-93,129 (peripherally acting)
  • CP-94,253
  • CP-122,288 (mixed 5-HT1B/1D agonist)
  • CP-135,807 (mixed 5-HT1B/1D agonist)
  • RU-24969 (mixed 5-HT1A/1B agonist)
  • Partial agonists

  • Vortioxetine (antidepressant)
  • Ziprasidone (antipsychotic)
  • Asenapine (antipsychotic)
  • Antagonists and inverse agonists

  • methiothepin (antipsychotic)
  • yohimbine (aphrodisiac)
  • metergoline
  • Aripiprazole
  • isamoltane
  • AR-A000002
  • SB-216,641
  • 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.

    References

    5-HT1B receptor Wikipedia


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