5-HT5A receptor
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5-HT5A receptor
5-hydroxytryptamine (serotonin) receptor 5A, also known as HTR5A, is a protein which in humans is encoded by the HTR5A gene.[1][2]
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Contents
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Function
The gene described in this record is a member of 5-hydroxytryptamine receptor family and encodes a multi-pass membrane protein that functions as a receptor for 5-hydroxytryptamine and couples to G proteins, negatively influencing cAMP levels via Gi and Go.[3] This protein has been shown to function in part through the regulation of intracellular Ca2+ mobilization.[1]
Rodents have been shown to possess two functional 5-HT5 receptor subtypes, 5-HT5A and 5-HT5B,[4] however while humans possess a gene coding for the 5-HT5B subtype, its coding sequence is interrupted by stop codons making the gene non-functional, and so only the 5-HT5A subtype is expressed in human brain.[5]
Clinical signficance
The neurotransmitter serotonin (5-hydroxytryptamine, 5-HT) has been implicated in a wide range of psychiatric conditions and also has vasoconstrictive and vasodilatory effects.[1]
Selective Ligands
Few highly selective ligands are commercially available for the 5-HT5A receptor. When selective activation of this receptor is desired in scientific research, the non-selective serotonin receptor agonist 5-Carboxamidotryptamine can be used in conjunction with selective antagonists for its other targets (principally 5-HT1A, 5-HT1B, 5-HT1D and 5-HT7). Research in this area is ongoing.[6][7]
Agonists
- Valerenic acid, a component of valerian, has been shown to act as a 5HT5A partial agonist.[8]
- Another ligand which has been recently disclosed is shown below, claimed be a selective 5-HT5A agonist with Ki = 124 nM.[9]
Antagonists
- Latrepirdine (non-selective)[10]
- SB-699,551
See also
References
- ^ a b c "Entrez Gene: HTR5A 5-hydroxytryptamine (serotonin) receptor 5A". http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=3361.
- ^ Rees S, den Daas I, Foord S, Goodson S, Bull D, Kilpatrick G, Lee M (December 1994). "Cloning and characterisation of the human 5-HT5A serotonin receptor". FEBS Lett. 355 (3): 242–6. doi:10.1016/0014-5793(94)01209-1. PMID 7988681.
- ^ Francken BJ, Jurzak M, Vanhauwe JF, Luyten WH, Leysen JE (November 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. doi:10.1016/S0014-2999(98)00744-4. PMID 9865521.
- ^ Matthes H, Boschert U, Amlaiky N, Grailhe R, Plassat JL, Muscatelli F, Mattei MG, Hen R (March 1993). "Mouse 5-hydroxytryptamine5A and 5-hydroxytryptamine5B receptors define a new family of serotonin receptors: cloning, functional expression, and chromosomal localization". Mol. Pharmacol. 43 (3): 313–9. PMID 8450829. http://molpharm.aspetjournals.org/cgi/reprint/43/3/313.
- ^ Nelson DL (February 2004). "5-HT5 receptors". Curr Drug Targets CNS Neurol Disord 3 (1): 53–8. doi:10.2174/1568007043482606. PMID 14965244.
- ^ Wesołowska A (2002). "In the search for selective ligands of 5-HT5, 5-HT6 and 5-HT7 serotonin receptors". Pol J Pharmacol 54 (4): 327–41. PMID 12523486. http://www.if-pan.krakow.pl/pjp/pdf/2002/4_327.pdf.
- ^ Peters JU, Lübbers T, Alanine A, Kolczewski S, Blasco F, Steward L (January 2008). "Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: optimising brain penetration". Bioorg. Med. Chem. Lett. 18 (1): 262–6. doi:10.1016/j.bmcl.2007.10.078. PMID 18023344.
- ^ Dietz BM, Mahady GB, Pauli GF, Farnsworth NR (August 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. doi:10.1016/j.molbrainres.2005.04.009. PMID 15921820.
- ^ Use of 5-HT5-ligands in the treatment of neurodegenerative and neuropsychiatric disturbances. 2004-06-15
- ^ Wu J, Li Q, Bezprozvanny I (2008). "Evaluation of Dimebon in cellular model of Huntington's disease". Mol Neurodegener 3 (1): 15. doi:10.1186/1750-1326-3-15. PMC 2577671. PMID 18939977. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2577671.
External links
- "5-ht5a". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2331.
Further reading
- Raymond JR, Mukhin YV, Gelasco A, et al. (2002). "Multiplicity of mechanisms of serotonin receptor signal transduction.". Pharmacol. Ther. 92 (2-3): 179–212. doi:10.1016/S0163-7258(01)00169-3. PMID 11916537.
- Thomas DR (2006). "5-ht5A receptors as a therapeutic target.". Pharmacol. Ther. 111 (3): 707–14. doi:10.1016/j.pharmthera.2005.12.006. PMID 16516972.
- Rees S, den Daas I, Foord S, et al. (1995). "Cloning and characterisation of the human 5-HT5A serotonin receptor.". FEBS Lett. 355 (3): 242–6. doi:10.1016/0014-5793(94)01209-1. PMID 7988681.
- 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. doi:10.1159/000134184. PMID 8978771.
- "Toward a complete human genome sequence.". Genome Res. 8 (11): 1097–108. 1999. doi:10.1101/gr.8.11.1097. PMID 9847074.
- Francken BJ, Josson K, Lijnen P, et al. (2000). "Human 5-hydroxytryptamine(5A) receptors activate coexpressed G(i) and G(o) proteins in Spodoptera frugiperda 9 cells.". Mol. Pharmacol. 57 (5): 1034–44. PMID 10779389.
- Marazziti D, Ori M, Nardini M, et al. (2001). "mRNA expression of serotonin receptors of type 2C and 5A in human resting lymphocytes.". Neuropsychobiology 43 (3): 123–6. doi:10.1159/000054878. PMID 11287788.
- 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. doi:10.1038/sj.mp.4000829. PMID 11317225.
- 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. doi:10.1016/S0014-2999(01)00933-5. PMID 11343685.
- Strausberg RL, Feingold EA, Grouse LH, et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. doi:10.1073/pnas.242603899. PMC 139241. PMID 12477932. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=139241.
- Noda M, Yasuda S, Okada M, et al. (2003). "Recombinant human serotonin 5A receptors stably expressed in C6 glioma cells couple to multiple signal transduction pathways.". J. Neurochem. 84 (2): 222–32. doi:10.1046/j.1471-4159.2003.01518.x. PMID 12558985.
- Scherer SW, Cheung J, MacDonald JR, et al. (2003). "Human chromosome 7: DNA sequence and biology.". Science 300 (5620): 767–72. doi:10.1126/science.1083423. PMC 2882961. PMID 12690205. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2882961.
- Hillier LW, Fulton RS, Fulton LA, et al. (2003). "The DNA sequence of human chromosome 7.". Nature 424 (6945): 157–64. doi:10.1038/nature01782. PMID 12853948.
- Khorana N, Smith C, Herrick-Davis K, et al. (2003). "Binding of tetrahydrocarboline derivatives at human 5-HT5A receptors.". J. Med. Chem. 46 (18): 3930–7. doi:10.1021/jm030080s. PMID 12930153.
- Ota T, Suzuki Y, Nishikawa T, et al. (2004). "Complete sequencing and characterization of 21,243 full-length human cDNAs.". Nat. Genet. 36 (1): 40–5. doi:10.1038/ng1285. PMID 14702039.
- Gerhard DS, Wagner L, Feingold EA, et al. (2004). "The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).". Genome Res. 14 (10B): 2121–7. doi:10.1101/gr.2596504. PMC 528928. PMID 15489334. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=528928.
- 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. doi:10.1016/j.molbrainres.2005.04.009. PMID 15921820.
This article incorporates text from the United States National Library of Medicine, which is in the public domain.
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