5-HT5A receptor
edit |
5-hydroxytryptamine (serotonin) receptor 5A | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Identifiers | |||||||||||||
Symbols | HTR5A; 5-HT5A; MGC138226 | ||||||||||||
External IDs | OMIM: 601305 MGI: 96283 HomoloGene: 22461 IUPHAR: 5-ht5a GeneCards: HTR5A Gene | ||||||||||||
| |||||||||||||
RNA expression pattern | |||||||||||||
250px | |||||||||||||
More reference expression data | |||||||||||||
Orthologs | |||||||||||||
Species | Human | Mouse | |||||||||||
Entrez | 3361 | 15563 | |||||||||||
Ensembl | ENSG00000157219 | ENSMUSG00000039106 | |||||||||||
UniProt | P47898 | Q3URB0 | |||||||||||
RefSeq (mRNA) | NM_024012 | NM_008314 | |||||||||||
RefSeq (protein) | NP_076917 | NP_032340 | |||||||||||
Location (UCSC) | Chr 7: 154.49 - 154.51 Mb | Chr 5: 28.17 - 28.19 Mb | |||||||||||
PubMed search | [1] | [2] |
5-hydroxytryptamine (serotonin) receptor 5A, also known as HTR5A, is a protein which in humans is encoded by the HTR5A gene.[1][2]
Contents
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
Cite error: Invalid <references>
tag;
parameter "group" is allowed only.
<references />
, or <references group="..." />
External links
- "5-ht5a". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
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. 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 Freely accessible. PMID 12477932.
- 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 Freely accessible. PMID 12690205.
- 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 Freely accessible. PMID 15489334.
- 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.
40x30px | This transmembrane receptor-related article is a stub. You can help ssf by expanding it. |
- ↑ 1.0 1.1 1.2 "Entrez Gene: HTR5A 5-hydroxytryptamine (serotonin) receptor 5A".
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ Wesołowska A (2002). "In the search for selective ligands of 5-HT5, 5-HT6 and 5-HT7 serotonin receptors" (PDF). Pol J Pharmacol. 54 (4): 327–41. PMID 12523486.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ Wu J, Li Q, Bezprozvanny I (2008). "Evaluation of Dimebon in cellular model of Huntington's disease". Mol Neurodegener. 3: 15. doi:10.1186/1750-1326-3-15. PMC 2577671 Freely accessible. PMID 18939977.