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
Symbols HTR1A; 5-HT1A; 5HT1a; ADRB2RL1; ADRBRL1
External IDs OMIM: 109760 MGI: 96273 HomoloGene: 20148
RNA expression pattern

More reference expression data
Orthologs
Human Mouse
Entrez 3350 15550
Ensembl ENSG00000178394 ENSMUSG00000021721
Uniprot P08908 Q8BGS4
Refseq NM_000524 (mRNA)
NP_000515 (protein)		 NM_008308 (mRNA)
NP_032334 (protein)
Location Chr 5: 63.29 - 63.29 Mb Chr 13: 106.56 - 106.57 Mb
Pubmed search [1] [2]

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.

Contents

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]

Agonists Antagonists

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]

See also

References

  1. ^ 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. 
  2. ^ "Entrez Gene: HTR1A 5-hydroxytryptamine (serotonin) receptor 1A".
  3. ^ 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:10.1016/0014-2999(95)00438-Q. PMID 7498295. 
  4. ^ 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:10.1016/S0006-8993(01)03297-8. PMID 11814436. 
  5. ^ Borg J, Andrée B, Soderstrom H, Farde L (November 2003). "The serotonin system and spiritual experiences". Am J Psychiatry 160 (11): 1965–9. doi:10.1176/appi.ajp.160.11.1965. PMID 14594742. 
  6. ^ 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:10.1016/S0197-0186(96)00124-6. PMID 9152998. 
  7. ^ 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").". 
  8. ^ 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. 
  9. ^ 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. 
  10. ^ 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:10.1017/S1461145707008218. PMID 18047755. 
  11. ^ 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:10.1097/00041444-199906000-00010. PMID 10412191. 

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:10.1017/S1461145704004845. 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:10.1080/15216540500167237. 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:10.1038/329075a0. 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:10.1038/335358a0. 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:10.1074/jbc.M201539200. PMID 11854302. 

This article incorporates text from the United States National Library of Medicine, which is in the public domain.

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v • d • e
Transmembrane receptor: G protein-coupled receptors
Class A: Rhodopsin like
α1 (A, B, D) • α2 (A, B, C) • β1 • β2 • β3
CysLT (1, 2) • LTB4 (1, 2) • FPRL1 • OXE • Prostaglandin (DP, EP (1, 2, 3, 4), PGF) • Prostacyclin • Thromboxane
B/W (1, 2) • FF (1, 2) • S • Y (1, 2, 4, 5)
GPR (1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 79, 82, 83, 84, 85, 87, 88, 92, 101, 103, 119, 120, 132, 135, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 172, 173, 174, 176, 177, 182)
Adenosine (A1, A2a, A2b, A3) • P2Y (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)
(all but 5-HT3) 5-HT1 (A, B, D, E, F) • 5-HT2 (A, B, C) • 5-HT (4, 5A, 6, 7)
Other
Acetylcholine (M1, M2, M3, M4, M5) • Adrenomedullin • Anaphylatoxin (C3a, C5a) • Angiotensin (1, 2) • Apelin • Bile acid • Bombesin (BRS3, GRPR, NMBR) • Bradykinin (B1, B2) • Cannabinoid (CB1, CB2) • Chemokine • Cholecystokinin (A, B) • Dopamine (D1, D2, D3, D4, D5) • EBI2 • Endothelin (A, B) • Estrogen • Formyl peptide (1, L1, L2) • Free fatty acid (1, 2, 3, 4) • FSH • Galanin (1, 2, 3) • Gonadotropin-releasing hormone (1, 2) • Ghrelin • Histamine (H1, H2, H3, H4) • Kisspeptin • Luteinizing hormone/choriogonadotropin • Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) • MAS (1, 1L, D, E, F, G, X1, X2, X3, X4) • Melanocortin (1, 2, 3, 4, 5) • MCHR (1, 2) • Melatonin (1A, 1B) • Motilin • Neuromedin (B, U (1, 2)) • Neurotensin (1, 2) • Opioid (Delta, Kappa, Mu, Nociceptin, but not Sigma) • Olfactory • Opsin (3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH) • Orexin (1, 2) • Oxytocin • Oxoglutarate • PAF • Prokineticin (1, 2) • Prolactin-releasing peptide • Protease-activated (1, 2, 3, 4) • Relaxin (1, 2, 3, 4) • Somatostatin (1, 2, 3, 4, 5) • SREB • Succinate • TAAR (1, 2, 3, 5, 6, 8, 9) • Tachykinin (1, 2, 3) • Thyrotropin • Thyrotropin-releasing hormone • Urotensin-II • Vasopressin (1A, 1B, 2)
Class B: Secretin like
GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 157)
Other
Class C: Metabotropic
glutamate / pheromone
TAS1R (1, 2, 3) • TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 38, 39, 40, 41, 43, 44, 45, 46, 47, 48, 49, 50)
Other
Calcium-sensing receptor • GABA B (1, 2) • Glutamate receptor (Metabotropic glutamate (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A • GPR (156, 158, 179) • RAIG (1, 2, 3, 4)
Frizzled / Smoothened
Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10) • Smoothened

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