5-HT1A receptor

5-hydroxytryptamine (serotonin) receptor 1A is a 5-HT₁ receptor."HTR1A" denotes the human gene encoding it.cite journal | author = Gilliam TC, Freimer NB, Kaufmann CA, Powchik PP, Bassett AS, Bengtsson U, Wasmuth JJ | title = Deletion mapping of DNA markers to a region of chromosome 5 that cosegregates with schizophrenia | journal = Genomics | volume = 5 | issue = 4 | pages = 940–4 | year = 1989 | month = November | pmid = 2591972 | url = | issn = ] cite web | title = Entrez Gene: HTR1A 5-hydroxytryptamine (serotonin) receptor 1A | url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=3350 | accessdate = ] 5-HT_1A acts on the CNS, where it induces neuronal inhibition and controls behaviour, such as sleep, feeding, thermoregulation, aggression, anxiety.

Ligands

The distribution of 5-HT_1A receptors in the human brain may be imaged with the positron emission tomography using the radioligand [¹¹C] WAY-100635.cite journal
author = Pike VW, McCarron JA, Lammerstma AA, Hume SP, Poole K, Grasby PM, Malizia A, Cliffe IA, Fletcher A, Bench CJ | title = First delineation of 5-HT_1A receptors in human brain with PET and [¹¹C] WAY-100635 | journal = Eur. J. Pharmacol. | volume = 283 | issue = 1-3 | pages = R1–3 | year = 1995 | pmid = 7498295 | doi = 10.1016/0014-2999(95)00438-Q] For example, one study has found increased 5-HT_1A binding in type 2 diabetes.cite journal
author = Price JC, Kelley DE, Ryan CM, Meltzer CC, Drevets WC, Mathis CA, Mazumdar S, Reynolds CF | title = Evidence of increased serotonin-1A receptor binding in type 2 diabetes: a positron emission tomography study | journal = Brain Res. | volume = 927 | issue = 1 | pages = 97–103 | year = 2002 | pmid = 11814436 | doi = 10.1016/S0006-8993(01)03297-8 ] Another PET study found a negative correlation between amount of 5-HT_1A binding in the raphe nuclei, hippocampus and neocortex and a self reported tendency to have spiritual experiences.cite journal | author = Borg J, Andrée B, Soderstrom H, Farde L | title = The serotonin system and spiritual experiences | journal = Am J Psychiatry | volume = 160 | issue = 11 | pages = 1965–9 | year = 2003 | month = November | pmid = 14594742 | doi = 10.1176/appi.ajp.160.11.1965 | url = ]

Labeled with tritium, WAY-100635 may also be used in autoradiography.cite journal
author = Burnet PW, Eastwood SL, Harrison PJ
title = [³H] WAY-100635 for 5-HT_1A receptor autoradiography in human brain: a comparison with [³H] 8-OH-DPAT and demonstration of increased binding in the frontal cortex in schizophrenia
journal = Neurochem. Int.
volume = 30
issue = 6
pages = 565–574
year = 1997
pmid = 9152998
doi = 10.1016/S0197-0186(96)00124-6]

Genetics

The receptor is coded by the "HTR1A" gene.There are several human polymorphisms associated with this gene.A 2007 review listed 27 single nucleotide polymorphisms (SNP).cite journal | author = Drago A, Ronchi DD, Serretti A | title = 5-HT_1A gene variants and psychiatric disorders: a review of current literature and selection of SNPs for future studies | journal = Int. J. Neuropsychopharmacol. | volume = 11 | issue = 5 | pages = 701–21 | year = 2008 | month = August | pmid = 18047755 | doi = 10.1017/S1461145707008218 | url = ] The most investigated SNPs are C(-1019)G (rs6295) (C-1018G,cite journal | author = Wu S, Comings DE | title = A common C-1018G polymorphism in the human 5-HT_1A receptor gene | journal = Psychiatr. Genet. | volume = 9 | issue = 2 | pages = 105–6 | year = 1999 | month = June | pmid = 10412191 | url = | doi = 10.1097/00041444-199906000-00010 ] Ile28Val (rs1799921), Arg219Leu (rs1800044) and Gly22Ser (rs1799920).Some of the other SNPs are Pro16Leu and Gly272Asp.

The gene variants have been studied in relation to psychiatric disorders with no definitive results.

ee also

* 5-HT₁ receptor
* 5-HT receptor

References

Further reading

PBB_Further_reading
citations =
*cite journal | author=el Mestikawy S, Fargin A, Raymond JR, "et al." |title=The 5-HT1A receptor: an overview of recent advances |journal=Neurochem. Res. |volume=16 |issue= 1 |pages= 1–10 |year= 1991 |pmid= 2052135 |doi=
*cite journal | author=Hensler JG |title=Regulation of 5-HT1A receptor function in brain following agonist or antidepressant administration |journal=Life Sci. |volume=72 |issue= 15 |pages= 1665–82 |year= 2003 |pmid= 12559389 |doi=
*cite journal | author=Van Oekelen D, Luyten WH, Leysen JE |title=5-HT2A and 5-HT2C receptors and their atypical regulation properties |journal=Life Sci. |volume=72 |issue= 22 |pages= 2429–49 |year= 2003 |pmid= 12650852 |doi=
*cite journal | author=Lesch KP, Gutknecht L |title=Focus on The 5-HT1A receptor: emerging role of a gene regulatory variant in psychopathology and pharmacogenetics |journal=Int. J. Neuropsychopharmacol. |volume=7 |issue= 4 |pages= 381–5 |year= 2005 |pmid= 15683551 |doi= 10.1017/S1461145704004845
*cite journal | author=Kalipatnapu S, Chattopadhyay A |title=Membrane protein solubilization: recent advances and challenges in solubilization of serotonin1A receptors |journal=IUBMB Life |volume=57 |issue= 7 |pages= 505–12 |year= 2006 |pmid= 16081372 |doi= 10.1080/15216540500167237
*cite journal | author=Varrault A, Bockaert J, Waeber C |title=Activation of 5-HT1A receptors expressed in NIH-3T3 cells induces focus formation and potentiates EGF effect on DNA synthesis |journal=Mol. Biol. Cell |volume=3 |issue= 9 |pages= 961–9 |year= 1992 |pmid= 1330092 |doi=
*cite journal | author=Levy FO, Gudermann T, Perez-Reyes E, "et al." |title=Molecular cloning of a human serotonin receptor (S12) with a pharmacological profile resembling that of the 5-HT1D subtype |journal=J. Biol. Chem. |volume=267 |issue= 11 |pages= 7553–62 |year= 1992 |pmid= 1559993 |doi=
*cite journal | author=Melmer G, Sherrington R, Mankoo B, "et al." |title=A cosmid clone for the 5HT1A receptor (HTR1A) reveals a TaqI RFLP that shows tight linkage to dna loci D5S6, D5S39, and D5S76 |journal=Genomics |volume=11 |issue= 3 |pages= 767–9 |year= 1992 |pmid= 1685484 |doi=
*cite journal | author=Parks CL, Chang LS, Shenk T |title=A polymerase chain reaction mediated by a single primer: cloning of genomic sequences adjacent to a serotonin receptor protein coding region |journal=Nucleic Acids Res. |volume=19 |issue= 25 |pages= 7155–60 |year= 1992 |pmid= 1766875 |doi=
*cite journal | author=Gilliam TC, Freimer NB, Kaufmann CA, "et al." |title=Deletion mapping of DNA markers to a region of chromosome 5 that cosegregates with schizophrenia |journal=Genomics |volume=5 |issue= 4 |pages= 940–4 |year= 1990 |pmid= 2591972 |doi=
*cite journal | author=Kobilka BK, Frielle T, Collins S, "et al." |title=An intronless gene encoding a potential member of the family of receptors coupled to guanine nucleotide regulatory proteins |journal=Nature |volume=329 |issue= 6134 |pages= 75–9 |year= 1987 |pmid= 3041227 |doi= 10.1038/329075a0
*cite journal | author=Fargin A, Raymond JR, Lohse MJ, "et al." |title=The genomic clone G-21 which resembles a beta-adrenergic receptor sequence encodes the 5-HT1A receptor |journal=Nature |volume=335 |issue= 6188 |pages= 358–60 |year= 1988 |pmid= 3138543 |doi= 10.1038/335358a0
*cite journal | author=Nakhai B, Nielsen DA, Linnoila M, Goldman D |title=Two naturally occurring amino acid substitutions in the human 5-HT1A receptor: glycine 22 to serine 22 and isoleucine 28 to valine 28 |journal=Biochem. Biophys. Res. Commun. |volume=210 |issue= 2 |pages= 530–6 |year= 1995 |pmid= 7755630 |doi=
*cite journal | author=Aune TM, McGrath KM, Sarr T, "et al." |title=Expression of 5HT1a receptors on activated human T cells. Regulation of cyclic AMP levels and T cell proliferation by 5-hydroxytryptamine |journal=J. Immunol. |volume=151 |issue= 3 |pages= 1175–83 |year= 1993 |pmid= 8393041 |doi=
*cite journal | author=Parks CL, Shenk T |title=The serotonin 1a receptor gene contains a TATA-less promoter that responds to MAZ and Sp1 |journal=J. Biol. Chem. |volume=271 |issue= 8 |pages= 4417–30 |year= 1996 |pmid= 8626793 |doi=
*cite journal | author=Stockmeier CA, Shapiro LA, Dilley GE, "et al." |title=Increase in serotonin-1A autoreceptors in the midbrain of suicide victims with major depression-postmortem evidence for decreased serotonin activity |journal=J. Neurosci. |volume=18 |issue= 18 |pages= 7394–401 |year= 1998 |pmid= 9736659 |doi=
*cite journal | author=Kawanishi Y, Harada S, Tachikawa H, "et al." |title=Novel mutations in the promoter and coding region of the human 5-HT1A receptor gene and association analysis in schizophrenia |journal=Am. J. Med. Genet. |volume=81 |issue= 5 |pages= 434–9 |year= 1998 |pmid= 9754630 |doi=
*cite journal | author=Salim K, Fenton T, Bacha J, "et al." |title=Oligomerization of G-protein-coupled receptors shown by selective co-immunoprecipitation |journal=J. Biol. Chem. |volume=277 |issue= 18 |pages= 15482–5 |year= 2002 |pmid= 11854302 |doi= 10.1074/jbc.M201539200

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