Protein kodiran genom je član familije 5-hidroksitriptaminskih receptora. Njegov endogeni ligand je 5-hidroksitriptamin. On snižava cAMP nivoe putem i proteina.[3] Za ovaj protein je pokazano da delom funkcioniše putem regulacije intracelularne mobilizacije 2+.[1]
Glodari imaju dva funkcionalna tipa 5-5 receptora, i ,[4] Ljudi takože imaju gen, ali njegova kodirajuća sekvenca sadrži stop kodone, tako da taj gen nije funkcionalan, i samo je izražen u ljudskom mozgu.[5]
Mali broj visoko selektivnih liganda je komercijalno dostupan za receptor. Selektivna aktivacija ovog receptora se može ostvariti korištenjem neselektivnog agonista serotoninskog receptor 5-karboksamidotriptamina u kombinaciji sa selektivnim antagonistima za druge ciljeve (primarno i ).[6][7]
Rees S, den Daas I, Foord S, Goodson S, Bull D, Kilpatrick G, Lee M (1994). „Cloning and characterisation of the human 5-HT5A serotonin receptor”. FEBS Lett. 355 (3): 242—6. PMID7988681. doi:10.1016/0014-5793(94)01209-1.
Francken BJ, Jurzak M, Vanhauwe JF, Luyten WH, Leysen JE (1998). „The human 5-ht5A receptor couples to Gi/Go proteins and inhibits adenylate cyclase in HEK 293 cells”. Eur. J. Pharmacol. 361 (2-3): 299—309. PMID9865521. doi:10.1016/S0014-2999(98)00744-4.
Dietz BM, Mahady GB, Pauli GF, Farnsworth NR (2005). „Valerian extract and valerenic acid are partial agonists of the 5-HT5a receptor in vitro”. Brain Res. Mol. Brain Res. 138 (2): 191—7. PMID15921820. doi:10.1016/j.molbrainres.2005.04.009.
Garcia-Ladona, Francisco Javier; Szabo, Laszlo; Steiner, Gerd; Hofmann, Hans-Peter (15. 06. 2004). „Use of 5-HT5-ligands in the treatment of neurodegenerative and neuropsychiatric disturbances”. patent-number 6750221.
Rees S; den Daas I; Foord S; . (1995). „Cloning and characterisation of the human 5-HT5A serotonin receptor.”. FEBS Lett. 355 (3): 242—6. PMID7988681. doi:10.1016/0014-5793(94)01209-1.
Schanen NC, Scherer SW, Tsui LC, Francke U (1997). „Assignment of the 5-hydroxytryptamine (serotonin) receptor 5A gene (HTR5A) to human chromosome band 7q36.1.”. Cytogenet. Cell Genet. 72 (2-3): 187—8. PMID8978771. doi:10.1159/000134184.
Marazziti D; Ori M; Nardini M; . (2001). „mRNA expression of serotonin receptors of type 2C and 5A in human resting lymphocytes.”. Neuropsychobiology. 43 (3): 123—6. PMID11287788. doi:10.1159/000054878.
Iwata N, Ozaki N, Inada T, Goldman D (2001). „Association of a 5-HT(5A) receptor polymorphism, Pro15Ser, to schizophrenia.”. Mol. Psychiatry. 6 (2): 217—9. PMID11317225. doi:10.1038/sj.mp.4000829.
Grailhe R, Grabtree GW, Hen R (2001). „Human 5-HT(5) receptors: the 5-HT(5A) receptor is functional but the 5-HT(5B) receptor was lost during mammalian evolution.”. Eur. J. Pharmacol. 418 (3): 157—67. PMID11343685. doi:10.1016/S0014-2999(01)00933-5.
Noda M; Yasuda S; Okada M; . (2003). „Recombinant human serotonin 5A receptors stably expressed in C6 glioma cells couple to multiple signal transduction pathways.”. J. Neurochem. 84 (2): 222—32. PMID12558985. doi:10.1046/j.1471-4159.2003.01518.x.
Hillier, LW; RS, Fulton; Fulton, LA; . (2003). „The DNA sequence of human chromosome 7.”. Nature. 424 (6945): 157—64. PMID12853948. doi:10.1038/nature01782.
Khorana N; Smith C; Herrick-Davis K; . (2003). „Binding of tetrahydrocarboline derivatives at human 5-HT5A receptors.”. J. Med. Chem. 46 (18): 3930—7. PMID12930153. doi:10.1021/jm030080s.
Ota T; Suzuki Y; Nishikawa T; . (2004). „Complete sequencing and characterization of 21,243 full-length human cDNAs.”. Nat. Genet. 36 (1): 40—5. PMID14702039. doi:10.1038/ng1285.
Dietz BM, Mahady GB, Pauli GF, Farnsworth NR (2005). „Valerian extract and valerenic acid are partial agonists of the 5-HT5a receptor in vitro.”. Brain Res. Mol. Brain Res. 138 (2): 191—7. PMID15921820. doi:10.1016/j.molbrainres.2005.04.009.
Spoljašnje veze
„5-ht5a”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Архивирано из оригинала 26. 02. 2014. г.
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