5-HT1B receptor

5-hydroxytryptamine (serotonin) receptor 1B
Identifiers
Symbols	HTR1B; 5-HT1B; 5-HT1DB; HTR1D2; HTR1DB; S12
External IDs	OMIM: 182131 MGI: 96274 HomoloGene: 669 GeneCards: HTR1B Gene
Gene Ontology Molecular function • receptor activity • G-protein coupled receptor activity • serotonin receptor activity • protein binding • drug binding • serotonin binding Cellular component • cytoplasm • plasma membrane • plasma membrane • integral to plasma membrane Biological process • G-protein coupled receptor internalization • G-protein coupled receptor protein signaling pathway • G-protein signaling, coupled to cyclic nucleotide second messenger • activation of protein kinase C activity by G-protein coupled receptor protein signaling pathway • synaptic transmission • regulation of dopamine secretion • negative regulation of cAMP biosynthetic process • negative regulation of synaptic transmission, GABAergic • response to cocaine • response to drug • drinking behavior • response to ethanol • bone remodeling • response to mineralocorticoid stimulus • negative regulation of synaptic transmission, glutamatergic • cellular response to temperature stimulus Sources: Amigo / QuickGO
RNA expression pattern
More reference expression data
Orthologs
Species	Human	Mouse
Entrez	3351	15551
Ensembl	ENSG00000135312	ENSMUSG00000049511
UniProt	P28222	Q0VES5
RefSeq (mRNA)	NM_000863	NM_010482.1
RefSeq (protein)	NP_000854	NP_034612.1
Location (UCSC)	Chr 6: 78.17 – 78.17 Mb	Chr 9: 81.52 – 81.53 Mb
PubMed search	[1]	[2]

5-hydroxytryptamine receptor 1B also known as the 5-HT_1B receptor is a protein that in humans is encoded by the HTR1B gene. The 5-HT_1B receptor is a 5-HT receptor subtype.

Tissue distribution and function

The 5-HT_1B 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-HT_1B receptor increases the number of osteoblasts, bone mass, and the bone formation rate.

5-HT_1B 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-HT_1B receptor is thought to act as an autoreceptor, inhibiting the release of serotonin.

Knockout mice lacking the 5-HT_1B gene have shown an increase of aggression and a higher preference for alcohol.

Ligands

Agonists

• ergotamine (vasoconstrictor in migraine)
• sumatriptan (vasoconstrictor in migraine)
• zolmitriptan
• 5-Carboxamidotryptamine
• CGS-12066A
• CP-93,129 (peripherally acting)
• CP-94,253
• CP-135,807 (mixed 5-HT_1B/1D agonist)
• RU-24969 (mixed 5-HT_1A/1B agonist)

Antagonists and inverse agonists

• methiothepin (antipsychotic)
• yohimbine (aphrodisiac)
• metergoline
• 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.

See also

• 5-HT₁ receptor
• 5-HT receptor

External links

• "5-HT_1B". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2312. 

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 49324. PMID 1351684. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=49324. 
• 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 48922. PMID 1565658. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=48922. 
• 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 139241. PMID 12477932. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=139241. 
• 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.