5-HT5A receptor

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Lua error in Module:Infobox_gene at line 33: attempt to index field 'wikibase' (a nil value). 5-Hydroxytryptamine (serotonin) receptor 5A, also known as HTR5A, is a protein that 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] The 5-HT5A receptor has been shown to be functional in a native expression system.[4]

Rodents have been shown to possess two functional 5-HT5 receptor subtypes, 5-HT5A and 5-HT5B,[5] 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.[6]

It also appears to serve as an presynaptic serotonin autoreceptor.[7]

Clinical significance

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.[8][9]

Agonists

  • Valerenic acid, a component of valerian, has been shown to act as a 5HT5A partial agonist.[10]
  • Another ligand that has been recently disclosed is shown below, claimed be a selective 5-HT5A agonist with Ki = 124 nM.[11]

DE19900637A1 5HT5A ligand.png

Antagonists

See also

References

  1. 1.0 1.1 1.2 "Entrez Gene: HTR5A 5-hydroxytryptamine (serotonin) receptor 5A".<templatestyles src="Module:Citation/CS1/styles.css"></templatestyles>
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  5. Matthes H, Boschert U, Amlaiky N, Grailhe R, Plassat JL, Muscatelli F, Mattei MG, Hen R (Mar 1993). "Mouse 5-hydroxytryptamine5A and 5-hydroxytryptamine5B receptors define a new family of serotonin receptors: cloning, functional expression, and chromosomal localization". Molecular Pharmacology. 43 (3): 313–9. PMID 8450829.<templatestyles src="Module:Citation/CS1/styles.css"></templatestyles>
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  8. Wesołowska A (2002). "In the search for selective ligands of 5-HT5, 5-HT6 and 5-HT7 serotonin receptors" (PDF). Polish Journal of Pharmacology. 54 (4): 327–41. PMID 12523486.<templatestyles src="Module:Citation/CS1/styles.css"></templatestyles>
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  11. Garcia-Ladona, Francisco Javier; Szabo, Laszlo; Steiner, Gerd; Hofmann, Hans-Peter (2004-06-15). "Use of 5-HT5-ligands in the treatment of neurodegenerative and neuropsychiatric disturbances". Patent US 6750221.<templatestyles src="Module:Citation/CS1/styles.css"></templatestyles>
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Further reading

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  • Francken BJ, Josson K, Lijnen P, Jurzak M, Luyten WH, Leysen JE (May 2000). "Human 5-hydroxytryptamine(5A) receptors activate coexpressed G(i) and G(o) proteins in Spodoptera frugiperda 9 cells". Molecular Pharmacology. 57 (5): 1034–44. PMID 10779389.<templatestyles src="Module:Citation/CS1/styles.css"></templatestyles>
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External links

  • "5-ht5a". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.<templatestyles src="Module:Citation/CS1/styles.css"></templatestyles>

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