5-hydroxytryptamine receptor 3A is a protein that in humans is encoded by the HTR3Agene.[1][2]
The product of this gene belongs to the ligand-gated ion channel receptor superfamily. This gene encodes subunit A of the type 3 receptor for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor causes fast, depolarizing responses in neurons after activation. The A subunit is the only one that can be expressed alone and forms homomers with a very low single channel conductance of 0.6pS. When combined with the B subunit and expressed as a heteromer, the single channel conductance increases immensely. Alternatively spliced transcript variants encoding different isoforms have been identified.[3]
↑Weiss B, Mertz A, Schrock E, Koenen M, Rappold G (Feb 1996). "Assignment of a human homolog of the mouse Htr3 receptor gene to chromosome 11q23.1-q23.2". Genomics. 29 (1): 304–5. doi:10.1006/geno.1995.1254. PMID8530095.
↑Kelley SP, Dunlop JI, Kirkness EF, Lambert JJ, Peters JA (Jul 2003). "A cytoplasmic region determines single-channel conductance in 5-HT3 receptors". Nature. 424 (6946): 321–4. doi:10.1038/nature01788. PMID12867984.
Miyake A, Mochizuki S, Takemoto Y, Akuzawa S (1995). "Molecular cloning of human 5-hydroxytryptamine3 receptor: heterogeneity in distribution and function among species". Mol. Pharmacol. 48 (3): 407–16. PMID7565620.
Uetz P, Abdelatty F, Villarroel A, et al. (1994). "Organisation of the murine 5-HT3 receptor gene and assignment to human chromosome 11". FEBS Lett. 339 (3): 302–6. doi:10.1016/0014-5793(94)80435-4. PMID8112471.
Belelli D, Balcarek JM, Hope AG, et al. (1996). "Cloning and functional expression of a human 5-hydroxytryptamine type 3AS receptor subunit". Mol. Pharmacol. 48 (6): 1054–62. PMID8848005.
Brüss M, Göthert M, Hayer M, Bönisch H (1999). "Molecular cloning of alternatively spliced human 5-HT3 receptor cDNAs". Ann. N. Y. Acad. Sci. 861: 234–5. doi:10.1111/j.1749-6632.1998.tb10196.x. PMID9928262.
Davies PA, Pistis M, Hanna MC, et al. (1999). "The 5-HT3B subunit is a major determinant of serotonin-receptor function". Nature. 397 (6717): 359–63. doi:10.1038/16941. PMID9950429.
Brüss M, Eucker T, Göthert M, Bönisch H (2000). "Exon-intron organization of the human 5-HT3A receptor gene". Neuropharmacology. 39 (2): 308–15. doi:10.1016/S0028-3908(99)00116-1. PMID10670426.
Marazziti D, Betti L, Giannaccini G, et al. (2002). "Distribution of [3H]GR65630 binding in human brain postmortem". Neurochem. Res. 26 (3): 187–90. doi:10.1023/A:1010939530412. PMID11495540.
Spier AD, Lummis SC (2003). "Immunological characterization of 5-HT3 receptor transmembrane topology". J. Mol. Neurosci. 18 (3): 169–78. doi:10.1385/JMN:18:3:169. PMID12059035.
Boyd GW, Low P, Dunlop JI, et al. (2002). "Assembly and cell surface expression of homomeric and heteromeric 5-HT3 receptors: the role of oligomerization and chaperone proteins". Mol. Cell. Neurosci. 21 (1): 38–50. doi:10.1006/mcne.2002.1160. PMID12359150.
Hapfelmeier G, Haseneder R, Lampadius K, et al. (2003). "Cloned human and murine serotonin(3A) receptors expressed in human embryonic kidney 293 cells display different single-channel kinetics". Neurosci. Lett. 335 (1): 44–8. doi:10.1016/S0304-3940(02)01156-4. PMID12457738.
Pick H, Preuss AK, Mayer M, et al. (2003). "Monitoring expression and clustering of the ionotropic 5HT3 receptor in plasma membranes of live biological cells". Biochemistry. 42 (4): 877–84. doi:10.1021/bi026576d. PMID12549905.
Choi S, Lee JH, Oh S, et al. (2003). "Effects of ginsenoside Rg2 on the 5-HT3A receptor-mediated ion current in Xenopus oocytes". Mol. Cells. 15 (1): 108–13. PMID12661769.
Boyd GW, Doward AI, Kirkness EF, et al. (2003). "Cell surface expression of 5-hydroxytryptamine type 3 receptors is controlled by an endoplasmic reticulum retention signal". J. Biol. Chem. 278 (30): 27681–7. doi:10.1074/jbc.M304938200. PMID12750374.
Sun H, Hu XQ, Moradel EM, et al. (2003). "Modulation of 5-HT3 receptor-mediated response and trafficking by activation of protein kinase C". J. Biol. Chem. 278 (36): 34150–7. doi:10.1074/jbc.M303584200. PMID12791692.
Maksay G, Bikádi Z, Simonyi M (2004). "Binding interactions of antagonists with 5-hydroxytryptamine3A receptor models". J. Recept. Signal Transduct. Res. 23 (2–3): 255–70. doi:10.1081/RRS-120025568. PMID14626451.
Kaiser R, Tremblay PB, Sezer O, et al. (2004). "Investigation of the association between 5-HT3A receptor gene polymorphisms and efficiency of antiemetic treatment with 5-HT3 receptor antagonists". Pharmacogenetics. 14 (5): 271–8. doi:10.1097/00008571-200405000-00001. PMID15115912.
Panicker S, Cruz H, Arrabit C, et al. (2004). "Minimal structural rearrangement of the cytoplasmic pore during activation of the 5-HT3A receptor". J. Biol. Chem. 279 (27): 28149–58. doi:10.1074/jbc.M403545200. PMID15131114.