5-HT1B receptor

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5-hydroxytryptamine (serotonin) receptor 1B
SymbolsHTR1B; 5-HT1B; 5-HT1DB; HTR1D2; HTR1DB; S12
External IDsOMIM182131 MGI96274 HomoloGene669 IUPHAR: 5-HT1B GeneCards: HTR1B Gene
RNA expression pattern
More reference expression data
RefSeq (mRNA)NM_000863NM_010482
RefSeq (protein)NP_000854NP_034612
Location (UCSC)Chr 6:
78.23 - 78.23 Mb
Chr 9:
81.43 - 81.43 Mb
PubMed search[1][2]

5-hydroxytryptamine receptor 1B also known as the 5-HT1B receptor is a protein that in humans is encoded by the HTR1B gene.[1][2] The 5-HT1B receptor is a 5-HT receptor subtype.[3]

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 vasoconstriction.

Blocking the 5-HT1B receptor increases the number of osteoblasts, bone mass, and the bone formation rate.[4]

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.[citation needed] 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.[citation needed]

Knockout mice lacking the 5-HT1B gene has shown an increase of aggression and a higher preference for alcohol.[5]



Antagonists and inverse agonists


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.[9]

See also


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External links

  • "5-HT1B". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. 

Further reading

  • Olivier B, van Oorschot R (2006). "5-HT1B receptors and aggression: a review". Eur. J. Pharmacol. 526 (1-3): 207–17. doi:10.1016/j.ejphar.2005.09.066. PMID 16310769. 
  • Hamblin MW, Metcalf MA, McGuffin RW, Karpells S (1992). "Molecular cloning and functional characterization of a human 5-HT1B serotonin receptor: a homologue of the rat 5-HT1B receptor with 5-HT1D-like pharmacological specificity". Biochem. Biophys. Res. Commun. 184 (2): 752–9. doi:10.1016/0006-291X(92)90654-4. PMID 1315531. 
  • Veldman SA, Bienkowski MJ (1992). "Cloning and pharmacological characterization of a novel human 5-hydroxytryptamine1D receptor subtype". Mol. Pharmacol. 42 (3): 439–44. PMID 1328844. 
  • Demchyshyn L, Sunahara RK, Miller K; et al. (1992). "A human serotonin 1D receptor variant (5HT1D beta) encoded by an intronless gene on chromosome 6". Proc. Natl. Acad. Sci. U.S.A. 89 (12): 5522–6. doi:10.1073/pnas.89.12.5522. PMC 49324Freely accessible. PMID 1351684. 
  • Levy FO, Gudermann T, Perez-Reyes E; et al. (1992). "Molecular cloning of a human serotonin receptor (S12) with a pharmacological profile resembling that of the 5-HT1D subtype". J. Biol. Chem. 267 (11): 7553–62. PMID 1559993. 
  • Weinshank RL, Zgombick JM, Macchi MJ; et al. (1992). "Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta". Proc. Natl. Acad. Sci. U.S.A. 89 (8): 3630–4. doi:10.1073/pnas.89.8.3630. PMC 48922Freely accessible. PMID 1565658. 
  • Mochizuki D, Yuyama Y, Tsujita R; et al. (1992). "Cloning and expression of the human 5-HT1B-type receptor gene". Biochem. Biophys. Res. Commun. 185 (2): 517–23. doi:10.1016/0006-291X(92)91655-A. PMID 1610347. 
  • Nöthen MM, Erdmann J, Shimron-Abarbanell D, Propping P (1995). "Identification of genetic variation in the human serotonin 1D beta receptor gene". Biochem. Biophys. Res. Commun. 205 (2): 1194–200. doi:10.1006/bbrc.1994.2792. PMID 7802650. 
  • Ng GY, George SR, Zastawny RL; et al. (1993). "Human serotonin1B receptor expression in Sf9 cells: phosphorylation, palmitoylation, and adenylyl cyclase inhibition". Biochemistry. 32 (43): 11727–33. doi:10.1021/bi00094a032. PMID 8218242. 
  • Bouchelet I, Cohen Z, Case B; et al. (1996). "Differential expression of sumatriptan-sensitive 5-hydroxytryptamine receptors in human trigeminal ganglia and cerebral blood vessels". Mol. Pharmacol. 50 (2): 219–23. PMID 8700126. 
  • Varnäs K, Hall H, Bonaventure P, Sedvall G (2001). "Autoradiographic mapping of 5-HT(1B) and 5-HT(1D) receptors in the post mortem human brain using [(3)H]GR 125743". Brain Res. 915 (1): 47–57. doi:10.1016/S0006-8993(01)02823-2. PMID 11578619. 
  • Salim K, Fenton T, Bacha J; et al. (2002). "Oligomerization of G-protein-coupled receptors shown by selective co-immunoprecipitation". J. Biol. Chem. 277 (18): 15482–5. doi:10.1074/jbc.+M201539200. PMID 11854302. 
  • Hasegawa Y, Higuchi S, Matsushita S, Miyaoka H (2002). "Association of a polymorphism of the serotonin 1B receptor gene and alcohol dependence with inactive aldehyde dehydrogenase-2". Journal of neural transmission (Vienna, Austria : 1996). 109 (4): 513–21. doi:10.1007/s007020200042. PMID 11956970. 
  • Hawi Z, Dring M, Kirley A; et al. (2003). "Serotonergic system and attention deficit hyperactivity disorder (ADHD): a potential susceptibility locus at the 5-HT(1B) receptor gene in 273 nuclear families from a multi-centre sample". Mol. Psychiatry. 7 (7): 718–25. doi:10.1038/sj.mp.4001048. PMID 12192616. 
  • Strausberg RL, Feingold EA, Grouse LH; et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. doi:10.1073/pnas.242603899. PMC 139241Freely accessible. PMID 12477932. 
  • Huang YY, Oquendo MA, Friedman JM; et al. (2003). "Substance abuse disorder and major depression are associated with the human 5-HT1B receptor gene (HTR1B) G861C polymorphism". Neuropsychopharmacology. 28 (1): 163–9. doi:10.1038/sj.npp.1300000. PMID 12496953. 
  • Quist JF, Barr CL, Schachar R; et al. (2003). "The serotonin 5-HT1B receptor gene and attention deficit hyperactivity disorder". Mol. Psychiatry. 8 (1): 98–102. doi:10.1038/sj.mp.4001244. PMID 12556913. 
  • Sinha R, Cloninger CR, Parsian A (2003). "Linkage disequilibrium and haplotype analysis between serotonin receptor 1B gene variations and subtypes of alcoholism". Am. J. Med. Genet. B Neuropsychiatr. Genet. 121 (1): 83–8. doi:10.1002/ajmg.b.20064. PMID 12898580. 

This article incorporates text from the United States National Library of Medicine, which is in the public domain.

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  3. "Entrez Gene: HTR1B 5-hydroxytryptamine (serotonin) receptor 1B". 
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  5. Hoyer D, Hannon JP, Martin GR (2002). "Molecular, pharmacological and functional diversity of 5-HT receptors". Pharmacol. Biochem. Behav. 71 (4): 533–54. doi:10.1016/S0091-3057(01)00746-8. PMID 11888546. 
  6. Hudzik TJ, Yanek M, Porrey T, Evenden J, Paronis C, Mastrangelo M, Ryan C, Ross S, Stenfors C. Behavioral pharmacology of AR-A000002, a novel, selective 5-hydroxytryptamine(1B) antagonist. Journal of Pharmacology and Experimental Therapeutics. 2003 Mar;304(3):1072-84. PMID 12604684
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  9. Tsai SJ, Wang YC, Chen JY, Hong CJ (2003). "Allelic variants of the tryptophan hydroxylase (A218C) and serotonin 1B receptor (A-161T) and personality traits". Neuropsychobiology. 48 (2): 68–71. doi:10.1159/000072879. PMID 14504413.