5-HT5A receptor

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5-hydroxytryptamine (serotonin) receptor 5A
Identifiers
SymbolsHTR5A; 5-HT5A; MGC138226
External IDsOMIM601305 MGI96283 HomoloGene22461 IUPHAR: 5-ht5a GeneCards: HTR5A Gene
RNA expression pattern
250px
More reference expression data
Orthologs
SpeciesHumanMouse
Entrez336115563
EnsemblENSG00000157219ENSMUSG00000039106
UniProtP47898Q3URB0
RefSeq (mRNA)NM_024012NM_008314
RefSeq (protein)NP_076917NP_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]

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

  • Another ligand which has been recently disclosed is shown below, claimed be a selective 5-HT5A agonist with Ki = 124 nM.[9]

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Antagonists

See also

References

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External links

  • "5-ht5a". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. 

Further reading

This article incorporates text from the United States National Library of Medicine, which is in the public domain.

  1. 1.0 1.1 1.2 "Entrez Gene: HTR5A 5-hydroxytryptamine (serotonin) receptor 5A". 
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  6. 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. 
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  10. 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 2577671Freely accessible. PMID 18939977.