5-HT5A receptor
Template:Infobox gene 5-Hydroxytryptamine (serotonin) receptor 5A, also known as HTR5A, is a protein that in humans is encoded by the HTR5A gene.[1][2] Agonists and antagonists for 5-HT receptors, as well as serotonin uptake inhibitors, present promnesic (memory-promoting) and/or anti-amnesic effects under different conditions, and 5-HT receptors are also associated with neural changes.
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 a 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, though the field has expanded considerably in recent years.[8][9] 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.[10][11]
Agonists
- LSD:(+)-lysergic acid.[12][13]
- LisurideTemplate:Snd partial agonist.[13]
- 5-CTTemplate:Snd full agonist.[13]
- MethylergometrineTemplate:Snd full agonist.[13]
- Valerenic acidTemplate:Snd a component of valerian, has been shown to act as a 5HT5A partial agonist.[14]
- OlanzapineTemplate:Snd an atypical antipsychotic.[15]
- Psilocin[16]
- Aripiprazole - an atypical antipsychotic
- Mirtazapine - an atypical antidepressant
- UCSF648 - selective 5-HT5A partial agonist
- Another ligand that has been recently disclosed is shown below, claimed be a selective 5-HT5A agonist with Ki = 124 nM.[17]
File:DE19900637A1 5HT5A ligand.png
Antagonists
- ASP5736[18][19]
- AS-2030680[18]
- AS-2674723[18]
- MS112Template:Snd selective potent antangonist.[13]
- Latrepirdine (non-selective).[20]
- RisperidoneTemplate:Snd (non-selective), moderate 206 nM affinity.
- SB-699,551
See also
- 5-HT receptor
- 5-HT1 receptor
- 5-HT2 receptor
- 5-HT3 receptor
- 5-HT4 receptor
- 5-HT6 receptor
- 5-HT7 receptor
References
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- ↑ Volk B, Nagy BJ, Vas S, Kostyalik D, Simig G, Bagdy G. Medicinal chemistry of 5-HT5A receptor ligands: a receptor subtype with unique therapeutical potential. Curr Top Med Chem. 2010;10(5):554-78. Script error: No such module "CS1 identifiers". Template:Pmid
- ↑ Kordylewski SK, Bugno R, Bojarski AJ, Podlewska S. Uncovering the unique characteristics of different groups of 5-HT5AR ligands with reference to their interaction with the target protein. Pharmacol Rep. 2024 Oct;76(5):1130-1146. Script error: No such module "CS1 identifiers". Template:Pmid
- ↑ Script error: No such module "Citation/CS1".
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- ↑ The RBI Handbook of Receptor Classification and Signal Transduction, page 114 (1995)Template:ISBN
- ↑ a b c d e Script error: No such module "Citation/CS1".
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- ↑ Roth BL, Driscol J. "PDSP Ki Database". Psychoactive Drug Screening Program (PDSP). University of North Carolina at Chapel Hill and the United States National Institute of Mental Health. Retrieved 14 August 2017.
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- ↑ <templatestyles src="Citation/styles.css"/>Template:Citation/make link, Garcia-Ladona FJ, Szabo L, Steiner G, Hofmann HP, "Use of 5-HT5-ligands in the treatment of neurodegenerative and neuropsychiatric disturbances", published Script error: No such module "auto date formatter".Script error: No such module "Check for unknown parameters".
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Further reading
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External links
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- Template:UCSC gene info
This article incorporates text from the United States National Library of Medicine, which is in the public domain.
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Template:Serotonergics