5-hydroxytryptamine receptor 2B

Details

Name
5-hydroxytryptamine receptor 2B
Synonyms
  • 5-HT-2B
  • Serotonin receptor 2B
Gene Name
HTR2B
Organism
Humans
Amino acid sequence
>lcl|BSEQ0016078|5-hydroxytryptamine receptor 2B
MALSYRVSELQSTIPEHILQSTFVHVISSNWSGLQTESIPEEMKQIVEEQGNKLHWAALL
ILMVIIPTIGGNTLVILAVSLEKKLQYATNYFLMSLAVADLLVGLFVMPIALLTIMFEAM
WPLPLVLCPAWLFLDVLFSTASIMHLCAISVDRYIAIKKPIQANQYNSRATAFIKITVVW
LISIGIAIPVPIKGIETDVDNPNNITCVLTKERFGDFMLFGSLAAFFTPLAIMIVTYFLT
IHALQKKAYLVKNKPPQRLTWLTVSTVFQRDETPCSSPEKVAMLDGSRKDKALPNSGDET
LMRRTSTIGKKSVQTISNEQRASKVLGIVFFLFLLMWCPFFITNITLVLCDSCNQTTLQM
LLEIFVWIGYVSSGVNPLVYTLFNKTFRDAFGRYITCNYRATKSVKTLRKRSSKIYFRNP
MAENSKFFKKHGIRNGINPAMYQSPMRLRSSTIQSSSIILLDTLLLTENEGDKTEEQVSY
V
Number of residues
481
Molecular Weight
54297.41
Theoretical pI
9.47
GO Classification
Functions
drug binding / G-protein alpha-subunit binding / GTPase activator activity / serotonin binding / serotonin receptor activity
Processes
activation of phospholipase C activity / behavior / calcium-mediated signaling / cardiac muscle hypertrophy / cellular calcium ion homeostasis / cellular response to amine stimulus / cellular response to serotonin / cellular response to temperature stimulus / cGMP biosynthetic process / embryonic morphogenesis / ERK1 and ERK2 cascade / G-protein coupled receptor internalization / G-protein coupled receptor signaling pathway / heart morphogenesis / hepatic stellate cell activation / inositol phosphate metabolic process / intestine smooth muscle contraction / ion transmembrane transport / negative regulation of apoptotic process / negative regulation of autophagy / negative regulation of cell death / neural crest cell differentiation / neural crest cell migration / phosphatidylinositol 3-kinase signaling / phosphorylation / positive regulation of cell division / positive regulation of cell proliferation / positive regulation of cytokine production / positive regulation of cytokine secretion / positive regulation of endothelial cell proliferation / positive regulation of ERK1 and ERK2 cascade / positive regulation of I-kappaB kinase/NF-kappaB signaling / positive regulation of MAP kinase activity / positive regulation of nitric-oxide synthase activity / positive regulation of phosphatidylinositol biosynthetic process / protein kinase C signaling / protein kinase C-activating G-protein coupled receptor signaling pathway / regulation of behavior / release of sequestered calcium ion into cytosol / response to drug / serotonin receptor signaling pathway / vasoconstriction
Components
cell junction / cytoplasm / dendrite / integral component of plasma membrane / neuronal cell body / plasma membrane / synapse
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling activates a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and down-stream signaling cascades and promotes the release of Ca(2+) ions from intracellular stores. Plays a role in the regulation of dopamine and 5-hydroxytryptamine release, 5-hydroxytryptamine uptake and in the regulation of extracellular dopamine and 5-hydroxytryptamine levels, and thereby affects neural activity. May play a role in the perception of pain. Plays a role in the regulation of behavior, including impulsive behavior. Required for normal proliferation of embryonic cardiac myocytes and normal heart development. Protects cardiomyocytes against apoptosis. Plays a role in the adaptation of pulmonary arteries to chronic hypoxia. Plays a role in vasoconstriction. Required for normal osteoblast function and proliferation, and for maintaining normal bone density. Required for normal proliferation of the interstitial cells of Cajal in the intestine.
Pfam Domain Function
Transmembrane Regions
57-79 91-113 130-151 172-192 217-239 325-345 361-382
Cellular Location
Cell membrane
Gene sequence
>lcl|BSEQ0016079|5-hydroxytryptamine receptor 2B (HTR2B)
ATGGCTCTCTCTTACAGAGTGTCTGAACTTCAAAGCACAATTCCTGAGCACATTTTGCAG
AGCACCTTTGTTCACGTTATCTCTTCTAACTGGTCTGGATTACAGACAGAATCAATACCA
GAGGAAATGAAACAGATTGTTGAGGAACAGGGAAATAAACTGCACTGGGCAGCTCTTCTG
ATACTCATGGTGATAATACCCACAATTGGTGGAAATACCCTTGTTATTCTGGCTGTTTCA
CTGGAGAAGAAGCTGCAGTATGCTACTAATTACTTTCTAATGTCCTTGGCGGTGGCTGAT
TTGCTGGTTGGATTGTTTGTGATGCCAATTGCCCTCTTGACAATAATGTTTGAGGCTATG
TGGCCCCTCCCACTTGTTCTATGTCCTGCCTGGTTATTTCTTGACGTTCTCTTTTCAACC
GCATCCATCATGCATCTCTGTGCCATTTCAGTGGATCGTTACATAGCCATCAAAAAGCCA
ATCCAGGCCAATCAATATAACTCACGGGCTACAGCATTCATCAAGATTACAGTGGTGTGG
TTAATTTCAATAGGCATTGCCATTCCAGTCCCTATTAAAGGGATAGAGACTGATGTGGAC
AACCCAAACAATATCACTTGTGTGCTGACAAAGGAACGTTTTGGCGATTTCATGCTCTTT
GGCTCACTGGCTGCCTTCTTCACACCTCTTGCAATTATGATTGTCACCTACTTTCTCACT
ATCCATGCTTTACAGAAGAAGGCTTACTTAGTCAAAAACAAGCCACCTCAACGCCTAACA
TGGTTGACTGTGTCTACAGTTTTCCAAAGGGATGAAACACCTTGCTCGTCACCGGAAAAG
GTGGCAATGCTGGATGGTTCTCGAAAGGACAAGGCTCTGCCCAACTCAGGTGATGAAACA
CTTATGCGAAGAACATCCACAATTGGGAAAAAGTCAGTGCAGACCATTTCCAACGAACAG
AGAGCCTCAAAGGTCCTAGGGATTGTGTTTTTCCTCTTTTTGCTTATGTGGTGTCCCTTC
TTTATTACAAATATAACTTTAGTTTTATGTGATTCCTGTAACCAAACTACTCTCCAAATG
CTCCTGGAGATATTTGTGTGGATAGGCTATGTTTCCTCAGGAGTGAATCCTTTGGTCTAC
ACCCTCTTCAATAAGACATTTCGGGATGCATTTGGCCGATATATCACCTGCAATTACCGG
GCCACAAAGTCAGTAAAAACTCTCAGAAAACGCTCCAGTAAGATCTACTTCCGGAATCCA
ATGGCAGAGAACTCTAAGTTTTTCAAGAAACATGGAATTCGAAATGGGATTAACCCTGCC
ATGTACCAGAGTCCAATGAGGCTCCGAAGTTCAACCATTCAGTCTTCATCAATCATTCTA
CTAGATACGCTTCTCCTCACTGAAAATGAAGGTGACAAAACTGAAGAGCAAGTTAGTTAT
GTATAG
Chromosome Location
2
Locus
2q36.3-q37.1
External Identifiers
ResourceLink
UniProtKB IDP41595
UniProtKB Entry Name5HT2B_HUMAN
GenBank Protein ID475198
GenBank Gene IDX77307
GenAtlas IDHTR2B
HGNC IDHGNC:5294
General References
  1. Schmuck K, Ullmer C, Engels P, Lubbert H: Cloning and functional characterization of the human 5-HT2B serotonin receptor. FEBS Lett. 1994 Mar 28;342(1):85-90. [PubMed:8143856]
  2. Choi DS, Birraux G, Launay JM, Maroteaux L: The human serotonin 5-HT2B receptor: pharmacological link between 5-HT2 and 5-HT1D receptors. FEBS Lett. 1994 Oct 3;352(3):393-9. [PubMed:7926008]
  3. Kursar JD, Nelson DL, Wainscott DB, Baez M: Molecular cloning, functional expression, and mRNA tissue distribution of the human 5-hydroxytryptamine2B receptor. Mol Pharmacol. 1994 Aug;46(2):227-34. [PubMed:8078486]
  4. Kim SJ, Veenstra-VanderWeele J, Hanna GL, Gonen D, Leventhal BL, Cook EH Jr: Mutation screening of human 5-HT(2B)receptor gene in early-onset obsessive-compulsive disorder. Mol Cell Probes. 2000 Feb;14(1):47-52. [PubMed:10722792]
  5. Ota T, Suzuki Y, Nishikawa T, Otsuki T, Sugiyama T, Irie R, Wakamatsu A, Hayashi K, Sato H, Nagai K, Kimura K, Makita H, Sekine M, Obayashi M, Nishi T, Shibahara T, Tanaka T, Ishii S, Yamamoto J, Saito K, Kawai Y, Isono Y, Nakamura Y, Nagahari K, Murakami K, Yasuda T, Iwayanagi T, Wagatsuma M, Shiratori A, Sudo H, Hosoiri T, Kaku Y, Kodaira H, Kondo H, Sugawara M, Takahashi M, Kanda K, Yokoi T, Furuya T, Kikkawa E, Omura Y, Abe K, Kamihara K, Katsuta N, Sato K, Tanikawa M, Yamazaki M, Ninomiya K, Ishibashi T, Yamashita H, Murakawa K, Fujimori K, Tanai H, Kimata M, Watanabe M, Hiraoka S, Chiba Y, Ishida S, Ono Y, Takiguchi S, Watanabe S, Yosida M, Hotuta T, Kusano J, Kanehori K, Takahashi-Fujii A, Hara H, Tanase TO, Nomura Y, Togiya S, Komai F, Hara R, Takeuchi K, Arita M, Imose N, Musashino K, Yuuki H, Oshima A, Sasaki N, Aotsuka S, Yoshikawa Y, Matsunawa H, Ichihara T, Shiohata N, Sano S, Moriya S, Momiyama H, Satoh N, Takami S, Terashima Y, Suzuki O, Nakagawa S, Senoh A, Mizoguchi H, Goto Y, Shimizu F, Wakebe H, Hishigaki H, Watanabe T, Sugiyama A, Takemoto M, Kawakami B, Yamazaki M, Watanabe K, Kumagai A, Itakura S, Fukuzumi Y, Fujimori Y, Komiyama M, Tashiro H, Tanigami A, Fujiwara T, Ono T, Yamada K, Fujii Y, Ozaki K, Hirao M, Ohmori Y, Kawabata A, Hikiji T, Kobatake N, Inagaki H, Ikema Y, Okamoto S, Okitani R, Kawakami T, Noguchi S, Itoh T, Shigeta K, Senba T, Matsumura K, Nakajima Y, Mizuno T, Morinaga M, Sasaki M, Togashi T, Oyama M, Hata H, Watanabe M, Komatsu T, Mizushima-Sugano J, Satoh T, Shirai Y, Takahashi Y, Nakagawa K, Okumura K, Nagase T, Nomura N, Kikuchi H, Masuho Y, Yamashita R, Nakai K, Yada T, Nakamura Y, Ohara O, Isogai T, Sugano S: Complete sequencing and characterization of 21,243 full-length human cDNAs. Nat Genet. 2004 Jan;36(1):40-5. Epub 2003 Dec 21. [PubMed:14702039]
  6. Hillier LW, Graves TA, Fulton RS, Fulton LA, Pepin KH, Minx P, Wagner-McPherson C, Layman D, Wylie K, Sekhon M, Becker MC, Fewell GA, Delehaunty KD, Miner TL, Nash WE, Kremitzki C, Oddy L, Du H, Sun H, Bradshaw-Cordum H, Ali J, Carter J, Cordes M, Harris A, Isak A, van Brunt A, Nguyen C, Du F, Courtney L, Kalicki J, Ozersky P, Abbott S, Armstrong J, Belter EA, Caruso L, Cedroni M, Cotton M, Davidson T, Desai A, Elliott G, Erb T, Fronick C, Gaige T, Haakenson W, Haglund K, Holmes A, Harkins R, Kim K, Kruchowski SS, Strong CM, Grewal N, Goyea E, Hou S, Levy A, Martinka S, Mead K, McLellan MD, Meyer R, Randall-Maher J, Tomlinson C, Dauphin-Kohlberg S, Kozlowicz-Reilly A, Shah N, Swearengen-Shahid S, Snider J, Strong JT, Thompson J, Yoakum M, Leonard S, Pearman C, Trani L, Radionenko M, Waligorski JE, Wang C, Rock SM, Tin-Wollam AM, Maupin R, Latreille P, Wendl MC, Yang SP, Pohl C, Wallis JW, Spieth J, Bieri TA, Berkowicz N, Nelson JO, Osborne J, Ding L, Meyer R, Sabo A, Shotland Y, Sinha P, Wohldmann PE, Cook LL, Hickenbotham MT, Eldred J, Williams D, Jones TA, She X, Ciccarelli FD, Izaurralde E, Taylor J, Schmutz J, Myers RM, Cox DR, Huang X, McPherson JD, Mardis ER, Clifton SW, Warren WC, Chinwalla AT, Eddy SR, Marra MA, Ovcharenko I, Furey TS, Miller W, Eichler EE, Bork P, Suyama M, Torrents D, Waterston RH, Wilson RK: Generation and annotation of the DNA sequences of human chromosomes 2 and 4. Nature. 2005 Apr 7;434(7034):724-31. [PubMed:15815621]
  7. 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. [PubMed:15489334]
  8. Ullmer C, Boddeke HG, Schmuck K, Lubbert H: 5-HT2B receptor-mediated calcium release from ryanodine-sensitive intracellular stores in human pulmonary artery endothelial cells. Br J Pharmacol. 1996 Mar;117(6):1081-8. [PubMed:8882600]
  9. Becamel C, Figge A, Poliak S, Dumuis A, Peles E, Bockaert J, Lubbert H, Ullmer C: Interaction of serotonin 5-hydroxytryptamine type 2C receptors with PDZ10 of the multi-PDZ domain protein MUPP1. J Biol Chem. 2001 Apr 20;276(16):12974-82. Epub 2001 Jan 9. [PubMed:11150294]
  10. Schaerlinger B, Hickel P, Etienne N, Guesnier L, Maroteaux L: Agonist actions of dihydroergotamine at 5-HT2B and 5-HT2C receptors and their possible relevance to antimigraine efficacy. Br J Pharmacol. 2003 Sep;140(2):277-84. Epub 2003 Aug 11. [PubMed:12970106]
  11. Nichols DE, Nichols CD: Serotonin receptors. Chem Rev. 2008 May;108(5):1614-41. doi: 10.1021/cr078224o. Epub 2008 May 14. [PubMed:18476671]
  12. Cussac D, Boutet-Robinet E, Ailhaud MC, Newman-Tancredi A, Martel JC, Danty N, Rauly-Lestienne I: Agonist-directed trafficking of signalling at serotonin 5-HT2A, 5-HT2B and 5-HT2C-VSV receptors mediated Gq/11 activation and calcium mobilisation in CHO cells. Eur J Pharmacol. 2008 Oct 10;594(1-3):32-8. doi: 10.1016/j.ejphar.2008.07.040. Epub 2008 Jul 30. [PubMed:18703043]
  13. Bevilacqua L, Doly S, Kaprio J, Yuan Q, Tikkanen R, Paunio T, Zhou Z, Wedenoja J, Maroteaux L, Diaz S, Belmer A, Hodgkinson CA, Dell'osso L, Suvisaari J, Coccaro E, Rose RJ, Peltonen L, Virkkunen M, Goldman D: A population-specific HTR2B stop codon predisposes to severe impulsivity. Nature. 2010 Dec 23;468(7327):1061-6. doi: 10.1038/nature09629. [PubMed:21179162]
  14. 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. [PubMed:20945968]
  15. 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. [PubMed:23519210]
  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. [PubMed:23519215]

Drug Relations

Drug Relations
DrugBank IDNameDrug groupPharmacological action?ActionsDetails
DB00216Eletriptanapproved, investigationalunknownagonistDetails
DB00508Triflupromazineapproved, vet_approvedyesantagonistDetails
DB00805MinaprineapprovedyesantagonistDetails
DB00574Fenfluramineapproved, illicit, investigational, withdrawnyesagonistDetails
DB01079Tegaserodapproved, investigational, withdrawnunknownantagonistDetails
DB01239Chlorprothixeneexperimental, investigational, withdrawnyesantagonistDetails
DB05461OPC-28326investigationalunknownDetails
DB05492Epicept NP-1investigationalunknownDetails
DB06216AsenapineapprovedunknownantagonistDetails
DB06229OcaperidoneinvestigationalunknownDetails
DB01186Pergolideapproved, investigational, vet_approved, withdrawnunknownagonistDetails
DB01200Bromocriptineapproved, investigationalunknownagonistDetails
DB00589Lisurideapproved, investigationalunknownantagonistDetails
DB00248CabergolineapprovedunknownagonistDetails
DB00413Pramipexoleapproved, investigationalunknownunknownDetails
DB00714Apomorphineapproved, investigationalunknownagonistDetails
DB00247MethysergideapprovedyesantagonistDetails
DB00320Dihydroergotamineapproved, investigationalunknownagonistDetails
DB01242Clomipramineapproved, investigational, vet_approvedyesantagonistDetails
DB01142Doxepinapproved, investigationalyesantagonistDetails
DB01454Midomafetamineexperimental, illicit, investigationalunknownagonistDetails
DB00370MirtazapineapprovedunknownbinderDetails
DB01392Yohimbineapproved, investigational, vet_approvedunknownantagonistDetails
DB00543AmoxapineapprovedunknownantagonistDetails
DB00334Olanzapineapproved, investigationalunknownantagonistDetails
DB06148Mianserinapproved, investigationalunknownbinderDetails
DB06016Cariprazineapproved, investigationalyesantagonistDetails
DB00696ErgotamineapprovedunknownDetails
DB00353MethylergometrineapprovedunknownDetails
DB04829Lysergic acid diethylamideillicit, investigational, withdrawnunknownagonistDetails
DB09286PipamperoneinvestigationalunknownDetails
DB06153PizotifenapprovedunknownantagonistDetails
DB05607PRX-08066investigationalunknownantagonistDetails
DB13025TiaprideinvestigationalyesantagonistDetails
DB09304SetiptilineexperimentalunknownantagonistDetails
DB13345Dihydroergocristineapproved, experimentalyesantagonistDetails
DB01049Ergoloid mesylateapprovedyesantagonistagonistDetails
DB11273DihydroergocornineapprovedyesantagonistagonistDetails
DB12141Gilteritinibapproved, investigationalnoinhibitorDetails
DB00477Chlorpromazineapproved, investigational, vet_approvedunknownbinderDetails
DB01221Ketamineapproved, vet_approvedunknownantagonistDetails
DB06678Esmirtazapineinvestigationalunknowninverse agonistDetails