5-hydroxytryptamine receptor 5A
From DrugPedia: A Wikipedia for Drug discovery
(→References) |
|||
| Line 104: | Line 104: | ||
{{G protein-coupled receptors}} | {{G protein-coupled receptors}} | ||
[[Category:G protein coupled receptors]] | [[Category:G protein coupled receptors]] | ||
| + | [[Category:HMRbase]] | ||
| + | |||
<!-- The PBB_Controls template provides controls for Protein Box Bot, please see Template:PBB_Controls for details. --> | <!-- The PBB_Controls template provides controls for Protein Box Bot, please see Template:PBB_Controls for details. --> | ||
Current revision
Contents |
[edit] Description
5-hydroxytryptamine (serotonin) receptor 5A, also known as HTR5A, is a protein which in humans is encoded by the HTR5A gene.<ref name="entrez">Template:Cite web</ref><ref name="pmid7988681">Rees S, den Daas I, Foord S, Goodson S, Bull D, Kilpatrick G, Lee M (December 1994). "[h Cloning and characterisation of the human 5-HT5A serotonin receptor]". FEBS Lett. 355 (3): 242–6. doi:. PMID 7988681.</ref>
[edit] General Characterstics
[edit] Source Organism
Cavia porcellus (Guinea pig).
[edit] Taxomomy
Eukaryota; Metazoa; Chordata; Craniata; Vertebrata; Euteleostomi;Mammalia; Eutheria; Euarchontoglires; Glires; Rodentia;Hystricognathi; Caviidae; Cavia.
[edit] Subcellular Localization
Membrane (By similarity).
[edit] Developmental Stage
[edit] Similarity
Belongs to the G-protein coupled receptor 1 family.
[edit] 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.<ref name="pmid9865521">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. PMID 9865521.</ref> This protein has been shown to function in part through the regulation of intracellular Ca2+ mobilization.<ref name="entrez"/>
Rodents have been shown to possess two functional 5-HT5 receptor subtypes, 5-HT5A and 5-HT5B,<ref name="pmid8450829">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.</ref> 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.<ref name="pmid14965244">Nelson DL (February 2004). "5-HT5 receptors". Curr Drug Targets CNS Neurol Disord 3 (1): 53–8. PMID 14965244.</ref>
[edit] 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.<ref name="entrez"/>
Categories:Receptors
Template:Wrongtitle
Template:PBB
[edit] 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.<ref name="pmid12523486">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.</ref><ref name="pmid18023344">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:. PMID 18023344.</ref>
Agonists
- Valerenic acid, a component of valerian, has been shown to act as a 5HT5A partial agonist.<ref name="pmid15921820">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:. PMID 15921820.</ref>
- Another ligand which has been recently disclosed is shown below, claimed be a selective 5-HT5A agonist with Ki = 124 nM.<ref name = "US6750221" >Template:Citation</ref>
Image:DE19900637A1 5HT5A ligand.png
[edit] Antagonists
[edit] See also
[edit] External links
[edit] References
Template:NLM content Template:Transmembranereceptor-stub Template:G protein-coupled receptorsTemplate:PBB Controls
