5-HT1A receptor
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The correct title of this article is 5-HT1A receptor. It appears incorrectly here because of technical restrictions.
5-hydroxytryptamine (serotonin) receptor 1A
Identifiers
External IDs OMIM: 109760 MGI: 96273 HomoloGene: 20148
Molecular function: • rhodopsin-like receptor activity
• receptor activity
• serotonin receptor activity
• receptor activity
• serotonin receptor activity
Cellular component: • integral to plasma membrane
• membrane
• membrane
Biological process: • signal transduction
• G-protein coupled receptor protein signaling pathway
• behavior
• positive regulation of cell proliferation
• G-protein coupled receptor protein signaling pathway
• behavior
• positive regulation of cell proliferation
RNA expression pattern
Orthologs
Human Mouse
5-hydroxytryptamine (serotonin) receptor 1A is a 5-HT1 receptor. HTR1A denotes the human gene encoding it.[1][2] 5-HT1A acts on the CNS, where it induces neuronal inhibition and controls behaviour, such as sleep, feeding, thermoregulation, aggression, anxiety.
[edit] Ligands
The distribution of 5-HT1A receptors in the human brain may be imaged with the positron emission tomography using the radioligand [11C]WAY-100635.[3] For example, one study has found increased 5-HT1A binding in type 2 diabetes.[4] Another PET study found a negative correlation between amount of 5-HT1A binding in the raphe nuclei, hippocampus and neocortex and a self reported tendency to have spiritual experiences.[5]
Labeled with tritium, WAY-100635 may also be used in autoradiography.[6]
[edit] 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).[10] The most investigated SNPs are C(-1019)G (rs6295) (C-1018G,[11] Ile28Val (rs1799921), Arg219Leu (rs1800044) and Gly22Ser (rs1799920).[10] Some of the other SNPs are Pro16Leu and Gly272Asp.
The gene variants have been studied in relation to psychiatric disorders with no definitive results.[10]
[edit] See also
[edit] References
^ Gilliam TC, Freimer NB, Kaufmann CA, Powchik PP, Bassett AS, Bengtsson U, Wasmuth JJ (November 1989). "Deletion mapping of DNA markers to a region of chromosome 5 that cosegregates with schizophrenia". Genomics 5 (4): 940–4. PMID 2591972. ^ "Entrez Gene: HTR1A 5-hydroxytryptamine (serotonin) receptor 1A". ^ Pike VW, McCarron JA, Lammerstma AA, Hume SP, Poole K, Grasby PM, Malizia A, Cliffe IA, Fletcher A, Bench CJ (1995). "First delineation of 5-HT1A receptors in human brain with PET and [11C]WAY-100635". Eur. J. Pharmacol. 283 (1-3): R1–3. doi:. PMID 7498295. ^ Price JC, Kelley DE, Ryan CM, Meltzer CC, Drevets WC, Mathis CA, Mazumdar S, Reynolds CF (2002). "Evidence of increased serotonin-1A receptor binding in type 2 diabetes: a positron emission tomography study". Brain Res. 927 (1): 97–103. doi:. PMID 11814436. ^ Borg J, Andrée B, Soderstrom H, Farde L (November 2003). "The serotonin system and spiritual experiences". Am J Psychiatry 160 (11): 1965–9. doi:. PMID 14594742. ^ Burnet PW, Eastwood SL, Harrison PJ (1997). "[3H]WAY-100635 for 5-HT1A receptor autoradiography in human brain: a comparison with [3H]8-OH-DPAT and demonstration of increased binding in the frontal cortex in schizophrenia". Neurochem. Int. 30 (6): 565–574. doi:. PMID 9152998. ^ Thompson MR, Callaghan PD, Hunt GE, Cornish JL, McGregor IS.. A role for oxytocin and 5-HT(1A) receptors in the prosocial effects of 3,4 methylenedioxymethamphetamine ("ecstasy")., http://www.mdma.net/oxytocin-release/index.html. ^ McCall RB, Romero AG, Bienkowski MJ, Harris DW, McGuire JC, Piercey MF, Shuck ME, Smith MW, Svensson KA, Schreur PJ, et al. (1994). "Characterization of U-92016A as a selective, orally active, high intrinsic activity 5-hydroxytryptamine1A agonist.". J. Pharmacol. Exp. Ther. 271 (2): 875-883. PMID 7965808, http://jpet.aspetjournals.org/cgi/content/abstract/271/2/875. ^ Fornal CA, Metzler CW, Gallegos RA, Veasey SC, McCreary AC, Jacobs BL (1996). "WAY-100635, a potent and selective 5-hydroxytryptamine1A antagonist, increases serotonergic neuronal activity in behaving cats: comparison with (S)-WAY-100135". J. Pharmacol. Exp. Ther. 278 (2): 752–62. PMID 8768728, http://jpet.aspetjournals.org/cgi/content/abstract/278/2/752. ^ a b c Drago A, Ronchi DD, Serretti A (August 2008). "5-HT1A gene variants and psychiatric disorders: a review of current literature and selection of SNPs for future studies". Int. J. Neuropsychopharmacol. 11 (5): 701–21. doi:. PMID 18047755. ^ Wu S, Comings DE (June 1999). "A common C-1018G polymorphism in the human 5-HT1A receptor gene". Psychiatr. Genet. 9 (2): 105–6. doi:. PMID 10412191.
[edit] Further reading
el Mestikawy S, Fargin A, Raymond JR, et al. (1991). "The 5-HT1A receptor: an overview of recent advances". Neurochem. Res. 16 (1): 1–10. PMID 2052135. Hensler JG (2003). "Regulation of 5-HT1A receptor function in brain following agonist or antidepressant administration". Life Sci. 72 (15): 1665–82. PMID 12559389. Van Oekelen D, Luyten WH, Leysen JE (2003). "5-HT2A and 5-HT2C receptors and their atypical regulation properties". Life Sci. 72 (22): 2429–49. PMID 12650852. Lesch KP, Gutknecht L (2005). "Focus on The 5-HT1A receptor: emerging role of a gene regulatory variant in psychopathology and pharmacogenetics". Int. J. Neuropsychopharmacol. 7 (4): 381–5. doi:. PMID 15683551. Kalipatnapu S, Chattopadhyay A (2006). "Membrane protein solubilization: recent advances and challenges in solubilization of serotonin1A receptors". IUBMB Life 57 (7): 505–12. doi:. PMID 16081372. Varrault A, Bockaert J, Waeber C (1992). "Activation of 5-HT1A receptors expressed in NIH-3T3 cells induces focus formation and potentiates EGF effect on DNA synthesis". Mol. Biol. Cell 3 (9): 961–9. PMID 1330092. Levy FO, Gudermann T, Perez-Reyes E, et al. (1992). "Molecular cloning of a human serotonin receptor (S12) with a pharmacological profile resembling that of the 5-HT1D subtype". J. Biol. Chem. 267 (11): 7553–62. PMID 1559993. Melmer G, Sherrington R, Mankoo B, et al. (1992). "A cosmid clone for the 5HT1A receptor (HTR1A) reveals a TaqI RFLP that shows tight linkage to dna loci D5S6, D5S39, and D5S76". Genomics 11 (3): 767–9. PMID 1685484. Parks CL, Chang LS, Shenk T (1992). "A polymerase chain reaction mediated by a single primer: cloning of genomic sequences adjacent to a serotonin receptor protein coding region". Nucleic Acids Res. 19 (25): 7155–60. PMID 1766875. Gilliam TC, Freimer NB, Kaufmann CA, et al. (1990). "Deletion mapping of DNA markers to a region of chromosome 5 that cosegregates with schizophrenia". Genomics 5 (4): 940–4. PMID 2591972. Kobilka BK, Frielle T, Collins S, et al. (1987). "An intronless gene encoding a potential member of the family of receptors coupled to guanine nucleotide regulatory proteins". Nature 329 (6134): 75–9. doi:. PMID 3041227. Fargin A, Raymond JR, Lohse MJ, et al. (1988). "The genomic clone G-21 which resembles a beta-adrenergic receptor sequence encodes the 5-HT1A receptor". Nature 335 (6188): 358–60. doi:. PMID 3138543. Nakhai B, Nielsen DA, Linnoila M, Goldman D (1995). "Two naturally occurring amino acid substitutions in the human 5-HT1A receptor: glycine 22 to serine 22 and isoleucine 28 to valine 28". Biochem. Biophys. Res. Commun. 210 (2): 530–6. PMID 7755630. Aune TM, McGrath KM, Sarr T, et al. (1993). "Expression of 5HT1a receptors on activated human T cells. Regulation of cyclic AMP levels and T cell proliferation by 5-hydroxytryptamine". J. Immunol. 151 (3): 1175–83. PMID 8393041. Parks CL, Shenk T (1996). "The serotonin 1a receptor gene contains a TATA-less promoter that responds to MAZ and Sp1". J. Biol. Chem. 271 (8): 4417–30. PMID 8626793. Stockmeier CA, Shapiro LA, Dilley GE, et al. (1998). "Increase in serotonin-1A autoreceptors in the midbrain of suicide victims with major depression-postmortem evidence for decreased serotonin activity". J. Neurosci. 18 (18): 7394–401. PMID 9736659. Kawanishi Y, Harada S, Tachikawa H, et al. (1998). "Novel mutations in the promoter and coding region of the human 5-HT1A receptor gene and association analysis in schizophrenia". Am. J. Med. Genet. 81 (5): 434–9. PMID 9754630. Salim K, Fenton T, Bacha J, et al. (2002). "Oligomerization of G-protein-coupled receptors shown by selective co-immunoprecipitation". J. Biol. Chem. 277 (18): 15482–5. doi:. PMID 11854302.
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