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
Symbol(s) HTR1A; 5-HT1A; 5HT1a; ADRB2RL1; ADRBRL1
External IDs OMIM: 109760 MGI96273 Homologene20148
RNA expression pattern

PBB GE HTR1A 221351 at tn.png

More reference expression data

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, also known as HTR1A, is a 5-HT1 receptor, but also denotes the human gene encoding it.[1] 5-HT1A acts on the CNS, where it induces neuronal inhibition and controls behaviour, such as sleep, feeding, thermoregulation, aggression, anxiety.


The distribution of 5-HT1A receptors in the human brain may be imaged with the positron emission tomography using the radioligand [11C]WAY-100635.[2] For example, one study has found increased 5-HT1A binding in type 2 diabetes.[3] 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.[4] Labeled with tritium, WAY-100635 may also be used in autoradiography.[5]

Agonists Antagonists

See also


  1. "Entrez Gene: HTR1A 5-hydroxytryptamine (serotonin) receptor 1A". 
  2. 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. PMID 7498295. doi:10.1016/0014-2999(95)00438-Q. 
  3. 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. PMID 11814436. doi:10.1016/S0006-8993(01)03297-8. 
  4. Borg J, Andrée B, Soderstrom H, Farde L (2003). "The serotonin system and spiritual experiences". Am J Psychiatry. 160 (11): 1965–9. PMID 14594742. doi:10.1176/appi.ajp.160.11.1965. 
  5. 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): 565–74. PMID 9152998. doi:10.1016/S0197-0186(96)00124-6. 
  6. 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. 

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. PMID 15683551. doi:10.1017/S1461145704004845. 
  • Kalipatnapu S, Chattopadhyay A (2006). "Membrane protein solubilization: recent advances and challenges in solubilization of serotonin1A receptors.". IUBMB Life. 57 (7): 505–12. PMID 16081372. doi:10.1080/15216540500167237. 
  • 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. PMID 3041227. doi:10.1038/329075a0. 
  • 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. PMID 3138543. doi:10.1038/335358a0. 
  • 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. PMID 11854302. doi:10.1074/jbc.M201539200. 

This article incorporates text from the United States National Library of Medicine, which is in the public domain. Template:Membrane-protein-stub