5-HT1B receptor

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5-hydroxytryptamine (serotonin) receptor 1B
Identifiers
SymbolsHTR1B; 5-HT1B; 5-HT1DB; HTR1D2; HTR1DB; S12
External IDsOMIM: 182131 MGI: 96274 HomoloGene: 669 IUPHAR: 5-HT1B GeneCards: HTR1B Gene
RNA expression pattern
250px
More reference expression data
Orthologs
SpeciesHumanMouse
Entrez335115551
EnsemblENSG00000135312ENSMUSG00000049511
UniProtP28222Q0VES5
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]

Ligands

Agonists

Antagonists and inverse agonists

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.[9]

See also

References

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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 49324 Freely 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 48922 Freely 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 139241 Freely 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.

Class A: Rhodopsin like
α1 (A, B, D) · α2 (A, B, C) · β1 · β2 · β3
Adenosine (A1, A2A, A2B, A3) · P2Y (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)
(all but 5-HT3) 5-HT1 (A, B, D, E, F) · 5-HT2 (A, B, C) · 5-HT (4, 5A, 6, 7)
Other
Acetylcholine (M1, M2, M3, M4, M5) · Dopamine (D1, D2, D3, D4, D5) · Histamine (H1, H2, H3, H4) · Melatonin (1A, 1B, 1C) · TAAR (1, 2, 3, 5, 6, 8, 9)
Metabolites and
signaling molecules
CysLT (1, 2) · LTB4 (1, 2) · FPRL1 · OXE · Prostaglandin (DP (1, 2), EP (1, 2, 3, 4), FP) · Prostacyclin · Thromboxane
Other
Bile acid · Cannabinoid (CB1, CB2, GPR (18, 55, 119)) · EBI2 · Estrogen · Free fatty acid (1, 2, 3, 4) · Lactate  · Lysophosphatidic acid (1, 2, 3, 4, 5, 6)  · Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) · Niacin (1, 2) · Oxoglutarate · PAF · Sphingosine-1-phosphate (1, 2, 3, 4, 5) · Succinate
Peptide
B/W (1, 2) · FF (1, 2) · S · Y (1, 2, 4, 5) · Neuromedin (B, U (1, 2)) · Neurotensin (1, 2)
Other
Miscellaneous
GPR (1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 81, 82, 83, 84, 85, 87, 88, 92, 101, 103, 109A, 109B, 119, 120, 132, 135, 137B, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 173, 174, 176, 177, 182, 183)
Other
Class B: Secretin like
GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 155, 157)
Other
Class C: Metabotropic
glutamate / pheromone
TAS1R (1, 2, 3) · TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 19, 20, 30, 31, 38, 39, 40, 41, 42, 43, 45, 46, 50)
Other
Class F:
Frizzled / Smoothened
Frizzled
Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10)
Smoothened
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  1. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  2. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  3. ↑ "Entrez Gene: HTR1B 5-hydroxytryptamine (serotonin) receptor 1B". 
  4. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  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
  7. ↑ Selkirk JV, Scott C, Ho M, Burton MJ, Watson J, Gaster LM, Collin L, Jones BJ, Middlemiss DN, Price GW. SB-224289--a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity. British Journal of Pharmacology. 1998 Sep;125(1):202-8. PMID 9776361
  8. ↑ Roberts C, Watson J, Price GW, Middlemiss DN. SB-236057-A: a selective 5-HT1B receptor inverse agonist. CNS Drug Reviews. 2001 Winter;7(4):433-44. PMID 11830759
  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. 
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