5-Hydroxytryptamine Receptor 2A (HTR2A)

5-HT2A; HTR2; Serotonin Receptor 2A

SPN	T295
HGNC	5293
MGI	109521
PubMed	17691947
RGD	61800
UniProt	P28223
Wiki	HTR2A

The mammalian receptor is a subtype of the 5-HT₂ receptor that belongs to the serotonin receptor family and is a G protein-coupled receptor (GPCR). This is the main excitatory receptor subtype among the GPCRs for serotonin (5-HT), although 5-HT_2A may also have an inhibitory effect on certain areas such as the visual cortex and the orbitofrontal cortex. This receptor was given importance first as the target of psychedelic drugs like LSD. Later it came back to prominence because it was also found to be mediating, at least partly, the action of many antipsychotic drugs, especially the atypical ones. 5-HT_2A also happens to be a necessary receptor for the spread of the human polyoma virus called JC virus. HTR2 gene consists of 3 exons separated by 2 introns and spans over 20 kb.

Reference

"Cloning of the human serotonin 5-HT2 and 5-HT1C receptor subtypes."
Biochem. Biophys. Res. Commun. 181:1469-1478(1991) [PubMed] [Europe PMC] [Abstract]

"The human 5-HT2 receptor is encoded by a multiple intron-exon gene."
Brain Res. Mol. Brain Res. 14:20-26(1992) [PubMed] [Europe PMC] [Abstract]

"Primary structure of the human platelet serotonin 5-HT2A receptor: identify with frontal cortex serotonin 5-HT2A receptor."
J. Neurochem. 63:465-469(1994) [PubMed] [Europe PMC] [Abstract]

"Complete sequencing and characterization of 21,243 full-length human cDNAs."
Nat. Genet. 36:40-45(2004) [PubMed] [Europe PMC] [Abstract]

"The DNA sequence and analysis of human chromosome 13."
Nature 428:522-528(2004) [PubMed] [Europe PMC] [Abstract]

"The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC)."
Genome Res. 14:2121-2127(2004) [PubMed] [Europe PMC] [Abstract]

"Genomic organization, coding sequence and functional expression of human 5-HT2 and 5-HT1A receptor genes."
Eur. J. Pharmacol. 227:153-162(1992) [PubMed] [Europe PMC] [Abstract]

"Interaction of serotonin 5-hydroxytryptamine type 2C receptors with PDZ10 of the multi-PDZ domain protein MUPP1."
J. Biol. Chem. 276:12974-12982(2001) [PubMed] [Europe PMC] [Abstract]

"The serotonin 5-HT2A and 5-HT2C receptors interact with specific sets of PDZ proteins."
J. Biol. Chem. 279:20257-20266(2004) [PubMed] [Europe PMC] [Abstract]

"Serotonin receptors."
Chem. Rev. 108:1614-1641(2008) [PubMed] [Europe PMC] [Abstract]

"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. 594:32-38(2008) [PubMed] [Europe PMC] [Abstract]

"Identification of a serotonin/glutamate receptor complex implicated in psychosis."
Nature 452:93-97(2008) [PubMed] [Europe PMC] [Abstract]

"Pharmacological characterization of mitogen-activated protein kinase activation by recombinant human 5-HT2C, 5-HT2A, and 5-HT2B receptors."
Naunyn Schmiedebergs Arch. Pharmacol. 379:461-471(2009) [PubMed] [Europe PMC] [Abstract]

"Functional crosstalk and heteromerization of serotonin 5-HT2A and dopamine D2 receptors."
Neuropharmacology 61:770-777(2011) [PubMed] [Europe PMC] [Abstract]

"Serotonin receptors - from molecular biology to clinical applications."
Physiol. Res. 60:15-25(2011) [PubMed] [Europe PMC] [Abstract]

"Heterocomplex formation of 5-HT2A-mGlu2 and its relevance for cellular signaling cascades."
Neuropharmacology 62:2184-2191(2012) [PubMed] [Europe PMC] [Abstract]

"Quantitative phosphoproteomics unravels biased phosphorylation of serotonin 2A receptor at Ser280 by hallucinogenic versus nonhallucinogenic agonists."
Mol. Cell. Proteomics 13:1273-1285(2014) [PubMed] [Europe PMC] [Abstract]

"Systematic screening for mutations in the human serotonin-2A (5-HT2A) receptor gene: identification of two naturally occurring receptor variants and association analysis in schizophrenia."
Hum. Genet. 97:614-619(1996) [PubMed] [Europe PMC] [Abstract]

"Unified approach to the analysis of genetic variation in serotonergic pathways."
Am. J. Med. Genet. 88:621-627(1999) [PubMed] [Europe PMC] [Abstract]

"Characterization of single-nucleotide polymorphisms in coding regions of human genes."
Nat. Genet. 22:231-238(1999) [PubMed] [Europe PMC] [Abstract]

Erratum
Nat. Genet. 23:373-373(1999)