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serotonin [5HT]-2A receptor; 5-hydroxytryptamine receptor 2A; 5-HT-2A; 5-HT-2; serotonin receptor 2A (HTR2A, HTR2)

Function: 1) G protein-coupled receptor that activates a PtdIns-Ca+2 second messenger system 2) tracheal smooth muscle contraction, bronchoconstriction 3) aldosterone production 4) interacts with MPDZ, INADL & possibly with MPP3, PRDX6, DLG4, DLG1, CASK, APBA1, AIP1 Structure: - belongs to the G-protein coupled receptor 1 family - PDZ domain-binding motif is involved in interactions with: INADL, CASK, APBA1, DLG1, DLG4. Compartment: - localizes to the post-synaptic thickening of axo-dendritic synapses Pharmacology: - likely involved in response to SSRI in the treatment of depression - HTR2A is downregulated by citalopram & probably other SSRIs - pimavanserin, a selective serotonin 5-HT2A receptor antagonist, is useful for treating psychosis associated with Parkinson's disease Polymorphism: - the A allele of SNP rs7997012 in the HTR2A gene confers likelihood of response to SSRIs [3] Laboratory: - HTR2A gene mutation - HTR2A+HTR2C gene mutation

General

glycoprotein serotonin [5HT]-2 receptor

Properties

SIZE: MW = 53 kD entity length = 471 aa COMPARTMENT: cellular membrane MOTIF: exoplasmic domain {1-75} MOTIF: N-glycosylation site {N8} N-glycosylation site {N38} N-glycosylation site {N44} N-glycosylation site {N51} N-glycosylation site {N54} transmembrane domain {76-99} cytoplasmic loop {100-110} transmembrane domain {111-132} exoplasmic loop {133-147} transmembrane domain {148-171} MOTIF: cysteine residue {C148} MODIFICATION: cysteine residue {C227} cytoplasmic loop {172-191} transmembrane domain {192-215} exoplasmic loop {216-233} MOTIF: cysteine residue {C227} MODIFICATION: cysteine residue {C148} transmembrane domain {234-254} cytoplasmic loop {255-324} transmembrane domain {325-346} exoplasmic loop {347-362} transmembrane domain {363-384} cytoplasmic domain {385-471}

Database Correlations

OMIM 182135 MORBIDMAP 182135 UniProt P28223 Pfam PF00001 Entrez Gene 3356 Kegg hsa:3356

References

  1. Entrez Gene :accession 3356
  2. Uniprot :accession P28223
  3. McMahon FJ, Buervenich S, Charney D, Lipsky R, Rush AJ, Wilson AF, Sorant AJ, Papanicolaou GJ, Laje G, Fava M, Trivedi MH, Wisniewski SR, Manji H. Variation in the gene encoding the serotonin 2A receptor is associated with outcome of antidepressant treatment. Am J Hum Genet. 2006 May;78(5):804-14. Epub 2006 Mar 20. PMID: 16642436
  4. SHMPD; Singapore human mutation and polymorphism database http://shmpd.bii.a-star.edu.sg/gene.php?genestart=A&genename=HTR2A