5-hydroxytryptamine receptor 1B

Details

Name
5-hydroxytryptamine receptor 1B
Synonyms
  • 5-HT-1B
  • 5-HT-1D-beta
  • HTR1DB
  • S12
  • Serotonin 1D beta receptor
  • Serotonin receptor 1B
Gene Name
HTR1B
Organism
Humans
Amino acid sequence
>lcl|BSEQ0019014|5-hydroxytryptamine receptor 1B
MEEPGAQCAPPPPAGSETWVPQANLSSAPSQNCSAKDYIYQDSISLPWKVLLVMLLALIT
LATTLSNAFVIATVYRTRKLHTPANYLIASLAVTDLLVSILVMPISTMYTVTGRWTLGQV
VCDFWLSSDITCCTASILHLCVIALDRYWAITDAVEYSAKRTPKRAAVMIALVWVFSISI
SLPPFFWRQAKAEEEVSECVVNTDHILYTVYSTVGAFYFPTLLLIALYGRIYVEARSRIL
KQTPNRTGKRLTRAQLITDSPGSTSSVTSINSRVPDVPSESGSPVYVNQVKVRVSDALLE
KKKLMAARERKATKTLGIILGAFIVCWLPFFIISLVMPICKDACWFHLAIFDFFTWLGYL
NSLINPIIYTMSNEDFKQAFHKLIRFKCTS
Number of residues
390
Molecular Weight
43567.535
Theoretical pI
8.82
GO Classification
Functions
drug binding / serotonin binding / serotonin receptor activity
Processes
adenylate cyclase-inhibiting serotonin receptor signaling pathway / bone remodeling / cellular response to alkaloid / cellular response to drug / cellular response to temperature stimulus / drinking behavior / G-protein coupled receptor internalization / G-protein coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger / negative regulation of cAMP biosynthetic process / negative regulation of serotonin secretion / negative regulation of synaptic transmission, GABAergic / negative regulation of synaptic transmission, glutamatergic / protein kinase C-activating G-protein coupled receptor signaling pathway / regulation of behavior / regulation of dopamine secretion / response to cocaine / response to ethanol / response to mineralocorticoid / synaptic transmission / vasoconstriction
Components
cytoplasm / integral component of plasma membrane / plasma membrane
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances, such as lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity. Arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Regulates the release of 5-hydroxytryptamine, dopamine and acetylcholine in the brain, and thereby affects neural activity, nociceptive processing, pain perception, mood and behavior. Besides, plays a role in vasoconstriction of cerebral arteries.
Pfam Domain Function
Transmembrane Regions
50-75 85-110 124-145 166-187 206-228 316-336 350-371
Cellular Location
Cell membrane
Gene sequence
>lcl|BSEQ0019015|5-hydroxytryptamine receptor 1B (HTR1B)
ATGGAGGAACCGGGTGCTCAGTGCGCTCCACCGCCGCCCGCGGGCTCCGAGACCTGGGTT
CCTCAAGCCAACTTATCCTCTGCTCCCTCCCAAAACTGCAGCGCCAAGGACTACATTTAC
CAGGACTCCATCTCCCTACCCTGGAAAGTACTGCTGGTTATGCTATTGGCGCTCATCACC
TTGGCCACCACGCTCTCCAATGCCTTTGTGATTGCCACAGTGTACCGGACCCGGAAACTG
CACACCCCGGCTAACTACCTGATCGCCTCTCTGGCGGTCACCGACCTGCTTGTGTCCATC
CTGGTGATGCCCATCAGCACCATGTACACTGTCACCGGCCGCTGGACACTGGGCCAGGTG
GTCTGTGACTTCTGGCTGTCGTCGGACATCACTTGTTGCACTGCCTCCATCCTGCACCTC
TGTGTCATCGCCCTGGACCGCTACTGGGCCATCACGGACGCCGTGGAGTACTCAGCTAAA
AGGACTCCCAAGAGGGCGGCGGTCATGATCGCGCTGGTGTGGGTCTTCTCCATCTCTATC
TCGCTGCCGCCCTTCTTCTGGCGTCAGGCTAAGGCCGAAGAGGAGGTGTCGGAATGCGTG
GTGAACACCGACCACATCCTCTACACGGTCTACTCCACGGTGGGTGCTTTCTACTTCCCC
ACCCTGCTCCTCATCGCCCTCTATGGCCGCATCTACGTAGAAGCCCGCTCCCGGATTTTG
AAACAGACGCCCAACAGGACCGGCAAGCGCTTGACCCGAGCCCAGCTGATAACCGACTCC
CCCGGGTCCACGTCCTCGGTCACCTCTATTAACTCGCGGGTTCCCGACGTGCCCAGCGAA
TCCGGATCTCCTGTGTATGTGAACCAAGTCAAAGTGCGAGTCTCCGACGCCCTGCTGGAA
AAGAAGAAACTCATGGCCGCTAGGGAGCGCAAAGCCACCAAGACCCTAGGGATCATTTTG
GGAGCCTTTATTGTGTGTTGGCTACCCTTCTTCATCATCTCCCTAGTGATGCCTATCTGC
AAAGATGCCTGCTGGTTCCACCTAGCCATCTTTGACTTCTTCACATGGCTGGGCTATCTC
AACTCCCTCATCAACCCCATAATCTATACCATGTCCAATGAGGACTTTAAACAAGCATTC
CATAAACTGATACGTTTTAAGTGCACAAGTTGA
Chromosome Location
6
Locus
6q13
External Identifiers
ResourceLink
UniProtKB IDP28222
UniProtKB Entry Name5HT1B_HUMAN
GenBank Protein ID219679
GenBank Gene IDD10995
GenAtlas IDHTR1B
HGNC IDHGNC:5287
General References
  1. Hamblin MW, Metcalf MA, McGuffin RW, Karpells S: 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. 1992 Apr 30;184(2):752-9. [Article]
  2. Mochizuki D, Yuyama Y, Tsujita R, Komaki H, Sagai H: Cloning and expression of the human 5-HT1B-type receptor gene. Biochem Biophys Res Commun. 1992 Jun 15;185(2):517-23. [Article]
  3. Jin H, Oksenberg D, Ashkenazi A, Peroutka SJ, Duncan AM, Rozmahel R, Yang Y, Mengod G, Palacios JM, O'Dowd BF: Characterization of the human 5-hydroxytryptamine1B receptor. J Biol Chem. 1992 Mar 25;267(9):5735-8. [Article]
  4. Levy FO, Gudermann T, Perez-Reyes E, Birnbaumer M, Kaumann AJ, Birnbaumer L: Molecular cloning of a human serotonin receptor (S12) with a pharmacological profile resembling that of the 5-HT1D subtype. J Biol Chem. 1992 Apr 15;267(11):7553-62. [Article]
  5. Weinshank RL, Zgombick JM, Macchi MJ, Branchek TA, Hartig PR: 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. 1992 Apr 15;89(8):3630-4. [Article]
  6. Demchyshyn L, Sunahara RK, Miller K, Teitler M, Hoffman BJ, Kennedy JL, Seeman P, Van Tol HH, Niznik HB: A human serotonin 1D receptor variant (5HT1D beta) encoded by an intronless gene on chromosome 6. Proc Natl Acad Sci U S A. 1992 Jun 15;89(12):5522-6. [Article]
  7. Veldman SA, Bienkowski MJ: Cloning and pharmacological characterization of a novel human 5-hydroxytryptamine1D receptor subtype. Mol Pharmacol. 1992 Sep;42(3):439-44. [Article]
  8. Kitano T, Liu YH, Ueda S, Saitou N: Human-specific amino acid changes found in 103 protein-coding genes. Mol Biol Evol. 2004 May;21(5):936-44. Epub 2004 Mar 10. [Article]
  9. Mungall AJ, Palmer SA, Sims SK, Edwards CA, Ashurst JL, Wilming L, Jones MC, Horton R, Hunt SE, Scott CE, Gilbert JG, Clamp ME, Bethel G, Milne S, Ainscough R, Almeida JP, Ambrose KD, Andrews TD, Ashwell RI, Babbage AK, Bagguley CL, Bailey J, Banerjee R, Barker DJ, Barlow KF, Bates K, Beare DM, Beasley H, Beasley O, Bird CP, Blakey S, Bray-Allen S, Brook J, Brown AJ, Brown JY, Burford DC, Burrill W, Burton J, Carder C, Carter NP, Chapman JC, Clark SY, Clark G, Clee CM, Clegg S, Cobley V, Collier RE, Collins JE, Colman LK, Corby NR, Coville GJ, Culley KM, Dhami P, Davies J, Dunn M, Earthrowl ME, Ellington AE, Evans KA, Faulkner L, Francis MD, Frankish A, Frankland J, French L, Garner P, Garnett J, Ghori MJ, Gilby LM, Gillson CJ, Glithero RJ, Grafham DV, Grant M, Gribble S, Griffiths C, Griffiths M, Hall R, Halls KS, Hammond S, Harley JL, Hart EA, Heath PD, Heathcott R, Holmes SJ, Howden PJ, Howe KL, Howell GR, Huckle E, Humphray SJ, Humphries MD, Hunt AR, Johnson CM, Joy AA, Kay M, Keenan SJ, Kimberley AM, King A, Laird GK, Langford C, Lawlor S, Leongamornlert DA, Leversha M, Lloyd CR, Lloyd DM, Loveland JE, Lovell J, Martin S, Mashreghi-Mohammadi M, Maslen GL, Matthews L, McCann OT, McLaren SJ, McLay K, McMurray A, Moore MJ, Mullikin JC, Niblett D, Nickerson T, Novik KL, Oliver K, Overton-Larty EK, Parker A, Patel R, Pearce AV, Peck AI, Phillimore B, Phillips S, Plumb RW, Porter KM, Ramsey Y, Ranby SA, Rice CM, Ross MT, Searle SM, Sehra HK, Sheridan E, Skuce CD, Smith S, Smith M, Spraggon L, Squares SL, Steward CA, Sycamore N, Tamlyn-Hall G, Tester J, Theaker AJ, Thomas DW, Thorpe A, Tracey A, Tromans A, Tubby B, Wall M, Wallis JM, West AP, White SS, Whitehead SL, Whittaker H, Wild A, Willey DJ, Wilmer TE, Wood JM, Wray PW, Wyatt JC, Young L, Younger RM, Bentley DR, Coulson A, Durbin R, Hubbard T, Sulston JE, Dunham I, Rogers J, Beck S: The DNA sequence and analysis of human chromosome 6. Nature. 2003 Oct 23;425(6960):805-11. [Article]
  10. Gerhard DS, Wagner L, Feingold EA, Shenmen CM, Grouse LH, Schuler G, Klein SL, Old S, Rasooly R, Good P, Guyer M, Peck AM, Derge JG, Lipman D, Collins FS, Jang W, Sherry S, Feolo M, Misquitta L, Lee E, Rotmistrovsky K, Greenhut SF, Schaefer CF, Buetow K, Bonner TI, Haussler D, Kent J, Kiekhaus M, Furey T, Brent M, Prange C, Schreiber K, Shapiro N, Bhat NK, Hopkins RF, Hsie F, Driscoll T, Soares MB, Casavant TL, Scheetz TE, Brown-stein MJ, Usdin TB, Toshiyuki S, Carninci P, Piao Y, Dudekula DB, Ko MS, Kawakami K, Suzuki Y, Sugano S, Gruber CE, Smith MR, Simmons B, Moore T, Waterman R, Johnson SL, Ruan Y, Wei CL, Mathavan S, Gunaratne PH, Wu J, Garcia AM, Hulyk SW, Fuh E, Yuan Y, Sneed A, Kowis C, Hodgson A, Muzny DM, McPherson J, Gibbs RA, Fahey J, Helton E, Ketteman M, Madan A, Rodrigues S, Sanchez A, Whiting M, Madari A, Young AC, Wetherby KD, Granite SJ, Kwong PN, Brinkley CP, Pearson RL, Bouffard GG, Blakesly RW, Green ED, Dickson MC, Rodriguez AC, Grimwood J, Schmutz J, Myers RM, Butterfield YS, Griffith M, Griffith OL, Krzywinski MI, Liao N, Morin R, Palmquist D, Petrescu AS, Skalska U, Smailus DE, Stott JM, Schnerch A, Schein JE, Jones SJ, Holt RA, Baross A, Marra MA, Clifton S, Makowski KA, Bosak S, Malek J: The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. 2004 Oct;14(10B):2121-7. [Article]
  11. Ng GY, George SR, Zastawny RL, Caron M, Bouvier M, Dennis M, O'Dowd BF: Human serotonin1B receptor expression in Sf9 cells: phosphorylation, palmitoylation, and adenylyl cyclase inhibition. Biochemistry. 1993 Nov 2;32(43):11727-33. [Article]
  12. Xie Z, Lee SP, O'Dowd BF, George SR: Serotonin 5-HT1B and 5-HT1D receptors form homodimers when expressed alone and heterodimers when co-expressed. FEBS Lett. 1999 Jul 30;456(1):63-7. [Article]
  13. Edvinsson L, Uddman E, Wackenfors A, Davenport A, Longmore J, Malmsjo M: Triptan-induced contractile (5-HT1B receptor) responses in human cerebral and coronary arteries: relationship to clinical effect. Clin Sci (Lond). 2005 Sep;109(3):335-42. [Article]
  14. Nichols DE, Nichols CD: Serotonin receptors. Chem Rev. 2008 May;108(5):1614-41. doi: 10.1021/cr078224o. Epub 2008 May 14. [Article]
  15. Pytliak M, Vargova V, Mechirova V, Felsoci M: Serotonin receptors - from molecular biology to clinical applications. Physiol Res. 2011;60(1):15-25. Epub 2010 Oct 15. [Article]
  16. Wacker D, Wang C, Katritch V, Han GW, Huang XP, Vardy E, McCorvy JD, Jiang Y, Chu M, Siu FY, Liu W, Xu HE, Cherezov V, Roth BL, Stevens RC: Structural features for functional selectivity at serotonin receptors. Science. 2013 May 3;340(6132):615-9. doi: 10.1126/science.1232808. Epub 2013 Mar 21. [Article]
  17. Wang C, Jiang Y, Ma J, Wu H, Wacker D, Katritch V, Han GW, Liu W, Huang XP, Vardy E, McCorvy JD, Gao X, Zhou XE, Melcher K, Zhang C, Bai F, Yang H, Yang L, Jiang H, Roth BL, Cherezov V, Stevens RC, Xu HE: Structural basis for molecular recognition at serotonin receptors. Science. 2013 May 3;340(6132):610-4. doi: 10.1126/science.1232807. Epub 2013 Mar 21. [Article]
  18. Nothen MM, Erdmann J, Shimron-Abarbanell D, Propping P: Identification of genetic variation in the human serotonin 1D beta receptor gene. Biochem Biophys Res Commun. 1994 Dec 15;205(2):1194-200. [Article]

Drug Relations

Drug Relations
DrugBank IDNameDrug groupPharmacological action?ActionsDetails
DB00216Eletriptanapproved, investigationalyesagonistDetails
DB00315Zolmitriptanapproved, investigationalyesagonistDetails
DB00952Naratriptanapproved, investigationalyesagonistDetails
DB00953RizatriptanapprovedyesagonistDetails
DB00998Frovatriptanapproved, investigationalyesagonistDetails
DB00320Dihydroergotamineapproved, investigationalyesagonistDetails
DB00669Sumatriptanapproved, investigationalyesagonistDetails
DB00696ErgotamineapprovedyesagonistDetails
DB00918Almotriptanapproved, investigationalunknownagonistDetails
DB00960Pindololapproved, investigationalunknownother/unknownligandDetails
DB04884DapoxetineinvestigationalunknownDetails
DB00571Propranololapproved, investigationalunknownother/unknownDetails
DB06096NXN-188investigationalunknownDetails
DB06216AsenapineapprovedunknownantagonistDetails
DB01186Pergolideapproved, investigational, vet_approved, withdrawnunknownagonistDetails
DB01200Bromocriptineapproved, investigational, withdrawnunknownagonistDetails
DB00589Lisurideapproved, investigationalunknownagonistDetails
DB00248CabergolineapprovedunknownagonistDetails
DB00714Apomorphineapproved, investigationalunknownagonistDetails
DB00246ZiprasidoneapprovedunknownantagonistDetails
DB00363ClozapineapprovedunknownantagonistDetails
DB01238Aripiprazoleapproved, investigationalunknownantagonistligandDetails
DB01224QuetiapineapprovedunknownligandDetails
DB01392Yohimbineapproved, investigational, vet_approvedunknownpartial agonistDetails
DB08807BopindololexperimentalunknownDetails
DB00904Ondansetronapproved, withdrawnunknownother/unknownDetails
DB00408LoxapineapprovedunknownbinderDetails
DB00543AmoxapineapprovedunknownantagonistDetails
DB00247MethysergideapprovedunknownbinderDetails
DB00321AmitriptylineapprovedunknownbinderDetails
DB01359Penbutololapproved, investigationalunknownantagonistDetails
DB09068Vortioxetineapproved, investigationalyespartial agonistDetails
DB06153PizotifenapprovedunknownantagonistDetails
DB14185Aripiprazole lauroxilapproved, investigationalunknownDetails
DB00935Oxymetazolineapproved, investigationalunknownagonistDetails
DB08804Nandrolone decanoateapproved, illicitunknownmodulatorDetails
DB13025TiaprideinvestigationalyesantagonistDetails
DB09304SetiptilineexperimentalunknownantagonistDetails
DB13345Dihydroergocristineapproved, experimentalyesantagonistDetails
DB01049Ergoloid mesylateapprovedyesantagonistagonistDetails
DB11273DihydroergocornineapprovedyesantagonistagonistDetails
DB12141Gilteritinibapproved, investigationalnoinhibitorDetails
DB00715Paroxetineapproved, investigationalunknownDetails
DB01239Chlorprothixeneapproved, experimental, investigational, withdrawnyesinhibitorDetails
DB01221Ketamineapproved, vet_approvedunknownantagonistDetails
DB00334Olanzapineapproved, investigationalunknowninhibitorDetails
DB12540LecozotaninvestigationalunknownregulatorDetails