5-hydroxytryptamine receptor 2B

Details

Name
5-hydroxytryptamine receptor 2B
Synonyms
  • 5-HT-2B
  • 5-HT2B
  • Serotonin receptor 2B
Gene Name
HTR2B
UniProtKB Entry
P41595Swiss-Prot
Organism
Humans
NCBI Taxonomy ID
9606
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
G protein-coupled serotonin receptor activity / Gq/11-coupled serotonin receptor activity / neurotransmitter receptor activity
Processes
cGMP-mediated signaling / chemical synaptic transmission / G protein-coupled receptor internalization / G protein-coupled receptor signaling pathway / G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger / G protein-coupled serotonin receptor signaling pathway / intracellular calcium ion homeostasis / phosphatidylinositol 3-kinase/protein kinase B signal transduction / phospholipase C-activating serotonin receptor signaling pathway / positive regulation of canonical NF-kappaB signal transduction / positive regulation of cell population proliferation / protein kinase C-activating G protein-coupled receptor signaling pathway / response to xenobiotic stimulus
Components
G protein-coupled serotonin receptor complex / nucleoplasm
General Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin) (PubMed:18703043, PubMed:23519210, PubMed:7926008, PubMed:8078486, PubMed:8143856, PubMed:8882600). Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances (PubMed:12970106, PubMed:18703043, PubMed:23519210, PubMed:23519215, PubMed:24357322, PubMed:28129538, PubMed:7926008, PubMed:8078486, PubMed:8143856). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors (PubMed:23519215, PubMed:28129538, PubMed:8078486, PubMed:8143856, PubMed:8882600). Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways (PubMed:23519215, PubMed:28129538). 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 (PubMed:18703043, PubMed:23519215, PubMed:28129538, PubMed:8078486, PubMed:8143856, PubMed:8882600). 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 (By similarity). Plays a role in the regulation of behavior, including impulsive behavior (PubMed:21179162). 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 (By similarity)
Specific Function
G protein-coupled serotonin receptor activity
Pfam Domain Function
Signal Regions
Not Available
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
2q37.1
External Identifiers
ResourceLink
UniProtKB IDP41595
UniProtKB Entry Name5HT2B_HUMAN
GenBank Protein ID475198
GenBank Gene IDX77307
GeneCard IDHTR2B
GenAtlas IDHTR2B
HGNC IDHGNC:5294
PDB ID(s)4IB4, 4NC3, 5TUD, 5TVN, 6DRX, 6DRY, 6DRZ, 6DS0, 7SRQ, 7SRR, 7SRS
KEGG IDhsa:3357
IUPHAR/Guide To Pharmacology ID7
NCBI Gene ID3357
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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
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  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. [Article]
  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. [Article]
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Associated Data

Bio-Entities
Bio-EntityType
5-hydroxytryptamine receptor 2B (Humans)protein
primary
Serotonin Receptors (Humans)protein
5-hydroxytryptamine 2 receptor (Humans)protein
5-hydroxytryptamine receptor 2 (Humans)protein
Drug Relations
DrugDrug groupPharmacological action?TypeActionsDetails
Triflupromazineapproved, vet_approvedyestargetantagonistDetails
MinaprineapprovedyestargetantagonistDetails
Fenfluramineapproved, illicit, investigational, withdrawnnotargetagonistDetails
Tegaserodapproved, investigational, withdrawnunknowntargetantagonistDetails
OPC-28326investigationalunknowntargetDetails
Epicept NP-1investigationalunknowntargetDetails
BF-1investigationalunknowntargetDetails
AsenapineapprovedunknowntargetantagonistDetails
OcaperidoneinvestigationalunknowntargetDetails
Pergolideapproved, investigational, vet_approved, withdrawnunknowntargetagonistDetails
Bromocriptineapproved, investigational, withdrawnunknowntargetagonistDetails
Lisurideapproved, investigationalunknowntargetantagonistDetails
CabergolineapprovedunknowntargetagonistDetails
Apomorphineapproved, investigationalunknowntargetagonistDetails
MethysergideapprovedyestargetantagonistDetails
Dihydroergotamineapproved, investigationalunknowntargetagonistDetails
Clomipramineapproved, investigational, vet_approvedyestargetantagonistDetails
Doxepinapproved, investigationalunknowntargetantagonistDetails
Midomafetamineexperimental, illicit, investigationalyestargetagonistDetails
Yohimbineapproved, investigational, vet_approvedunknowntargetantagonistDetails
AmoxapineapprovedunknowntargetantagonistDetails
Mianserinapproved, investigationalunknowntargetbinderDetails
ErgotamineapprovedunknowntargetDetails
MethylergometrineapprovedunknowntargetDetails
Lysergic acid diethylamideillicit, investigational, withdrawnunknowntargetagonistDetails
PipamperoneinvestigationalunknowntargetDetails
PizotifenapprovedunknowntargetantagonistDetails
PRX-08066investigationalunknowntargetantagonistDetails
Paroxetineapproved, investigationalunknowntargetagonistDetails
CyclobenzaprineapprovedunknowntargetantagonistDetails
Aripiprazoleapproved, investigationalunknowntargetinverse agonistDetails
Zolmitriptanapproved, investigationalnotargetagonistDetails
CyproheptadineapprovedunknowntargetantagonistDetails
Cariprazineapproved, investigationalunknowntargetantagonistDetails
Viloxazineapproved, investigational, withdrawnyestargetantagonistDetails
Brexpiprazoleapproved, investigationalunknowntargetantagonistDetails
Dihydro-alpha-ergocryptineapprovedyestargetagonistDetails
PiribedilinvestigationalyestargetantagonistDetails
m-ChlorophenylpiperazineinvestigationalyestargetagonistDetails
Serotonininvestigational, nutraceuticalyestargetinhibitorDetails
5-methoxy-N,N-dimethyltryptamineexperimental, illicityestargetinhibitorDetails
RitanserininvestigationalyestargetantagonistDetails
FendilinewithdrawnyestargetinhibitorDetails
VabicaserininvestigationalyestargetmodulatorDetails
MetergolineapprovedyestargetantagonistDetails
TiaprideinvestigationalyestargetantagonistDetails
SetiptilineexperimentalunknowntargetantagonistDetails
Dihydroergocristineapproved, experimentalyestargetantagonistDetails
Ergoloid mesylateapprovedyestargetantagonistagonistDetails
DihydroergocornineapprovedyestargetantagonistagonistDetails
Gilteritinibapproved, investigationalnotargetinhibitorDetails
Paroxetineapproved, investigationalunknowntargetDetails
Chlorprothixeneapproved, experimental, investigational, withdrawnyestargetinhibitorDetails
Chlorpromazineapproved, investigational, vet_approvedunknowntargetbinderDetails
Nandrolone decanoateapproved, illicitunknowntargetmodulatorDetails
Ketamineapproved, vet_approvedunknowntargetantagonistDetails
Esmirtazapineinvestigationalunknowntargetinverse agonistDetails