5-hydroxytryptamine receptor 2C

Details

Name
5-hydroxytryptamine receptor 2C
Synonyms
  • 5-HT-1C
  • 5-HT-2C
  • 5-HT1C
  • 5-hydroxytryptamine receptor 1C
  • HTR1C
  • Serotonin receptor 2C
Gene Name
HTR2C
Organism
Humans
Amino acid sequence
>lcl|BSEQ0001064|5-hydroxytryptamine receptor 2C
MVNLRNAVHSFLVHLIGLLVWQCDISVSPVAAIVTDIFNTSDGGRFKFPDGVQNWPALSI
VIIIIMTIGGNILVIMAVSMEKKLHNATNYFLMSLAIADMLVGLLVMPLSLLAILYDYVW
PLPRYLCPVWISLDVLFSTASIMHLCAISLDRYVAIRNPIEHSRFNSRTKAIMKIAIVWA
ISIGVSVPIPVIGLRDEEKVFVNNTTCVLNDPNFVLIGSFVAFFIPLTIMVITYCLTIYV
LRRQALMLLHGHTEEPPGLSLDFLKCCKRNTAEEENSANPNQDQNARRRKKKERRPRGTM
QAINNERKASKVLGIVFFVFLIMWCPFFITNILSVLCEKSCNQKLMEKLLNVFVWIGYVC
SGINPLVYTLFNKIYRRAFSNYLRCNYKVEKKPPVRQIPRVAATALSGRELNVNIYRHTN
EPVIEKASDNEPGIEMQVENLELPVNPSSVVSERISSV
Number of residues
458
Molecular Weight
51820.705
Theoretical pI
9.11
GO Classification
Functions
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding / drug binding / Gq/11-coupled serotonin receptor activity / serotonin binding / serotonin receptor activity
Processes
behavioral fear response / cellular calcium ion homeostasis / cGMP biosynthetic process / feeding behavior / locomotory behavior / phospholipase C-activating G-protein coupled receptor signaling pathway / phospholipase C-activating serotonin receptor signaling pathway / positive regulation of cytosolic calcium ion concentration involved in phospholipase C-activating G-protein coupled signaling pathway / positive regulation of ERK1 and ERK2 cascade / positive regulation of fat cell differentiation / positive regulation of phosphatidylinositol biosynthetic process / regulation of appetite / regulation of corticotropin-releasing hormone secretion / regulation of neurological system process / release of sequestered calcium ion into cytosol / response to drug / serotonin receptor signaling pathway / synaptic transmission
Components
cytosol / 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 various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-iodophenyl-2-aminopropane (DOI) and 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. 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. Regulates neuronal activity via the activation of short transient receptor potential calcium channels in the brain, and thereby modulates the activation of pro-opiomelacortin neurons and the release of CRH that then regulates the release of corticosterone. Plays a role in the regulation of appetite and eating behavior, responses to anxiogenic stimuli and stress. Plays a role in insulin sensitivity and glucose homeostasis.
Pfam Domain Function
Transmembrane Regions
53-78 90-110 128-150 171-193 214-235 312-333 349-371
Cellular Location
Cell membrane
Gene sequence
>lcl|BSEQ0010373|5-hydroxytryptamine receptor 2C (HTR2C)
ATGGTGAACCTGAGGAATGCGGTGCATTCATTCCTTGTGCACCTAATTGGCCTATTGGTT
TGGCAATGTGATATTTCTGTGAGCCCAGTAGCAGCTATAGTAACTGACATTTTCAATACC
TCCGATGGTGGACGCTTCAAATTCCCAGACGGGGTACAAAACTGGCCAGCACTTTCAATC
GTCATCATAATAATCATGACAATAGGTGGCAACATCCTTGTGATCATGGCAGTAAGCATG
GAAAAGAAACTGCACAATGCCACCAATTACTTCTTAATGTCCCTAGCCATTGCTGATATG
CTAGTGGGACTACTTGTCATGCCCCTGTCTCTCCTGGCAATCCTTTATGATTATGTCTGG
CCACTACCTAGATATTTGTGCCCCGTCTGGATTTCTTTAGATGTTTTATTTTCAACAGCG
TCCATCATGCACCTCTGCGCTATATCGCTGGATCGGTATGTAGCAATACGTAATCCTATT
GAGCATAGCCGTTTCAATTCGCGGACTAAGGCCATCATGAAGATTGCTATTGTTTGGGCA
ATTTCTATAGGTGTATCAGTTCCTATCCCTGTGATTGGACTGAGGGACGAAGAAAAGGTG
TTCGTGAACAACACGACGTGCGTGCTCAACGACCCAAATTTCGTTCTTATTGGGTCCTTC
GTAGCTTTCTTCATACCGCTGACGATTATGGTGATTACGTATTGCCTGACCATCTACGTT
CTGCGCCGACAAGCTTTGATGTTACTGCACGGCCACACCGAGGAACCGCCTGGACTAAGT
CTGGATTTCCTGAAGTGCTGCAAGAGGAATACGGCCGAGGAAGAGAACTCTGCAAACCCT
AACCAAGACCAGAACGCACGCCGAAGAAAGAAGAAGGAGAGACGTCCTAGGGGCACCATG
CAGGCTATCAACAATGAAAGAAAAGCTTCGAAAGTCCTTGGGATTGTTTTCTTTGTGTTT
CTGATCATGTGGTGCCCATTTTTCATTACCAATATTCTGTCTGTTCTTTGTGAGAAGTCC
TGTAACCAAAAGCTCATGGAAAAGCTTCTGAATGTGTTTGTTTGGATTGGCTATGTTTGT
TCAGGAATCAATCCTCTGGTGTATACTCTGTTCAACAAAATTTACCGAAGGGCATTCTCC
AACTATTTGCGTTGCAATTATAAGGTAGAGAAAAAGCCTCCTGTCAGGCAGATTCCAAGA
GTTGCCGCCACTGCTTTGTCTGGGAGGGAGCTTAATGTTAACATTTATCGGCATACCAAT
GAACCGGTGATCGAGAAAGCCAGTGACAATGAGCCCGGTATAGAGATGCAAGTTGAGAAT
TTAGAGTTACCAGTAAATCCCTCCAGTGTGGTTAGCGAAAGGATTAGCAGTGTGTGA
Chromosome Location
X
Locus
Xq24
External Identifiers
ResourceLink
UniProtKB IDP28335
UniProtKB Entry Name5HT2C_HUMAN
GenBank Protein ID338028
GenBank Gene IDM81778
GenAtlas IDHTR2C
HGNC IDHGNC:5295
General References
  1. Saltzman AG, Morse B, Whitman MM, Ivanshchenko Y, Jaye M, Felder S: Cloning of the human serotonin 5-HT2 and 5-HT1C receptor subtypes. Biochem Biophys Res Commun. 1991 Dec 31;181(3):1469-78. [PubMed:1722404]
  2. Stam NJ, Vanderheyden P, van Alebeek C, Klomp J, de Boer T, van Delft AM, Olijve W: Genomic organisation and functional expression of the gene encoding the human serotonin 5-HT2C receptor. Eur J Pharmacol. 1994 Nov 15;269(3):339-48. [PubMed:7895773]
  3. Xie E, Zhu L, Zhao L, Chang LS: The human serotonin 5-HT2C receptor: complete cDNA, genomic structure, and alternatively spliced variant. Genomics. 1996 Aug 1;35(3):551-61. [PubMed:8812491]
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Drug Relations

Drug Relations
DrugBank IDNameDrug groupPharmacological action?ActionsDetails
DB00574Fenfluramineapproved, illicit, investigational, withdrawnyesagonistDetails
DB00246ZiprasidoneapprovedunknownantagonistDetails
DB00334Olanzapineapproved, investigationalunknownantagonistDetails
DB00370MirtazapineapprovedunknownantagonistDetails
DB00420Promazineapproved, vet_approvedunknownantagonistDetails
DB00777PropiomazineapprovedunknownantagonistDetails
DB00805MinaprineapprovedyesantagonistDetails
DB01224QuetiapineapprovedunknownligandDetails
DB00193Tramadolapproved, investigationalunknownantagonistDetails
DB00363ClozapineapprovedunknownantagonistDetails
DB01191Dexfenfluramineapproved, illicit, investigational, withdrawnunknownagonistDetails
DB01239Chlorprothixeneapproved, experimental, investigational, withdrawnyesantagonistDetails
DB00247MethysergideapprovedyesantagonistDetails
DB04871LorcaserinapprovedunknownDetails
DB04884DapoxetineinvestigationalunknownDetails
DB06144Sertindoleapproved, investigational, withdrawnyesantagonistDetails
DB06148Mianserinapproved, investigationalunknownantagonistDetails
DB05492Epicept NP-1investigationalunknownDetails
DB06216AsenapineapprovedunknownantagonistDetails
DB06229OcaperidoneinvestigationalunknownDetails
DB12177EplivanserininvestigationalunknownDetails
DB06512Deramciclaneinvestigationalunknowninverse agonistDetails
DB06446DotarizineinvestigationalunknownDetails
DB06594Agomelatineapproved, investigationalyesantagonistDetails
DB01186Pergolideapproved, investigational, vet_approved, withdrawnunknownagonistDetails
DB01200Bromocriptineapproved, investigationalunknownagonistDetails
DB00589Lisurideapproved, investigationalyesagonistDetails
DB00248CabergolineapprovedunknownagonistDetails
DB00714Apomorphineapproved, investigationalunknownagonistDetails
DB00734Risperidoneapproved, investigationalunknownantagonistDetails
DB01267PaliperidoneapprovedyesantagonistDetails
DB01238Aripiprazoleapproved, investigationalunknownantagonistpartial agonistDetails
DB01403Methotrimeprazineapproved, investigationalunknownantagonistDetails
DB00656Trazodoneapproved, investigationalyesagonistDetails
DB00408LoxapineapprovedunknownantagonistDetails
DB00434CyproheptadineapprovedyesantagonistDetails
DB01392Yohimbineapproved, investigational, vet_approvedunknownantagonistDetails
DB01242Clomipramineapproved, investigational, vet_approvedyesantagonistDetails
DB01142Doxepinapproved, investigationalunknownantagonistDetails
DB01079Tegaserodapproved, investigational, withdrawnunknownantagonistDetails
DB01149Nefazodoneapproved, withdrawnyesantagonistDetails
DB01454Midomafetamineexperimental, illicit, investigationalunknownagonistDetails
DB00477Chlorpromazineapproved, investigational, vet_approvedunknownbinderDetails
DB00458ImipramineapprovedunknownantagonistbinderDetails
DB00543AmoxapineapprovedunknownantagonistDetails
DB00540NortriptylineapprovedunknownantagonistDetails
DB00726TrimipramineapprovedunknownantagonistDetails
DB00696ErgotamineapprovedunknownagonistDetails
DB00321AmitriptylineapprovedunknownantagonistDetails
DB00934Maprotilineapproved, investigationalunknownbinderDetails
DB01151Desipramineapproved, investigationalunknownbinderDetails
DB09014CaptodiameexperimentalyesantagonistDetails
DB12163SarpogrelateinvestigationalunknownDetails
DB00623FluphenazineapprovedunknownDetails
DB00472Fluoxetineapproved, vet_approvedunknownantagonistDetails
DB015374-Bromo-2,5-dimethoxyphenethylamineexperimental, illicityespartial agonistDetails
DB09194EtoperidonewithdrawnyesagonistDetails
DB139402,5-Dimethoxy-4-ethylthioamphetamineexperimentalunknownagonistDetails
DB09195LorpiprazoleapprovedyesantagonistDetails
DB12110m-ChlorophenylpiperazineinvestigationalunknownagonistDetails
DB06153PizotifenapprovedunknownantagonistDetails
DB04948Lofexidineapproved, investigationalnoagonistDetails
DB14185Aripiprazole lauroxilapproved, investigationalunknownDetails
DB00502HaloperidolapprovedyesDetails
DB00924CyclobenzaprineapprovedunknownantagonistDetails
DB01175EscitalopramapprovedunknowninhibitorDetails
DB13025TiaprideinvestigationalyesantagonistDetails
DB09304SetiptilineexperimentalunknownantagonistDetails
DB13345Dihydroergocristineapproved, experimentalyesantagonistDetails
DB01049Ergoloid mesylateapprovedyesantagonistagonistDetails
DB11273DihydroergocornineapprovedyesantagonistagonistDetails
DB12141Gilteritinibapproved, investigationalnoinhibitorDetails
DB00715Paroxetineapproved, investigationalunknownDetails
DB00477Chlorpromazineapproved, investigational, vet_approvedunknownbinderDetails
DB01221Ketamineapproved, vet_approvedunknownantagonistDetails
DB06678Esmirtazapineinvestigationalunknowninverse agonistDetails