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
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Identifiers | ||||||||||||||
Symbol(s) | HTR1A; 5-HT1A; 5HT1a; ADRB2RL1; ADRBRL1 | |||||||||||||
External IDs | OMIM: 109760 MGI: 96273 HomoloGene: 20148 | |||||||||||||
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RNA expression pattern | ||||||||||||||
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) |
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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.
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[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.[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 |
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[edit] See also
[edit] References
- ^ 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 (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): 565–74. doi: . PMID 9152998.
- ^ 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.
[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.
This article incorporates text from the United States National Library of Medicine, which is in the public domain.