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Discriminating between 5-HT(3)A and 5-HT(3)AB receptors

The 5-HT3B subunit was first cloned in 1999, and co-expression with the 5-HT3A subunit results in heteromeric 5-HT(3)AB receptors that are functionally distinct from homomeric 5-HT(3)A receptors. The affinities of competitive ligands at the two receptor subtypes are usually similar, but those of non...

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Detalles Bibliográficos
Autores principales: Thompson, AJ, Lummis, SCR
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Blackwell Publishing Ltd 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3687655/
https://www.ncbi.nlm.nih.gov/pubmed/23489111
http://dx.doi.org/10.1111/bph.12166
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author Thompson, AJ
Lummis, SCR
author_facet Thompson, AJ
Lummis, SCR
author_sort Thompson, AJ
collection PubMed
description The 5-HT3B subunit was first cloned in 1999, and co-expression with the 5-HT3A subunit results in heteromeric 5-HT(3)AB receptors that are functionally distinct from homomeric 5-HT(3)A receptors. The affinities of competitive ligands at the two receptor subtypes are usually similar, but those of non-competitive antagonists that bind in the pore often differ. A competitive ligand and allosteric modulator that distinguishes 5-HT(3)A from 5-HT(3)AB receptors has recently been described, and the number of non-competitive antagonists identified with this ability has increased in recent years. In this review, we discuss the differences between 5-HT(3)A and 5-HT(3)AB receptors and describe the possible sites of action of compounds that can distinguish between them.
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spelling pubmed-36876552013-11-03 Discriminating between 5-HT(3)A and 5-HT(3)AB receptors Thompson, AJ Lummis, SCR Br J Pharmacol Reviews The 5-HT3B subunit was first cloned in 1999, and co-expression with the 5-HT3A subunit results in heteromeric 5-HT(3)AB receptors that are functionally distinct from homomeric 5-HT(3)A receptors. The affinities of competitive ligands at the two receptor subtypes are usually similar, but those of non-competitive antagonists that bind in the pore often differ. A competitive ligand and allosteric modulator that distinguishes 5-HT(3)A from 5-HT(3)AB receptors has recently been described, and the number of non-competitive antagonists identified with this ability has increased in recent years. In this review, we discuss the differences between 5-HT(3)A and 5-HT(3)AB receptors and describe the possible sites of action of compounds that can distinguish between them. Blackwell Publishing Ltd 2013-06 2013-05-27 /pmc/articles/PMC3687655/ /pubmed/23489111 http://dx.doi.org/10.1111/bph.12166 Text en British Journal of Pharmacology © 2013 The British Pharmacological Society
spellingShingle Reviews
Thompson, AJ
Lummis, SCR
Discriminating between 5-HT(3)A and 5-HT(3)AB receptors
title Discriminating between 5-HT(3)A and 5-HT(3)AB receptors
title_full Discriminating between 5-HT(3)A and 5-HT(3)AB receptors
title_fullStr Discriminating between 5-HT(3)A and 5-HT(3)AB receptors
title_full_unstemmed Discriminating between 5-HT(3)A and 5-HT(3)AB receptors
title_short Discriminating between 5-HT(3)A and 5-HT(3)AB receptors
title_sort discriminating between 5-ht(3)a and 5-ht(3)ab receptors
topic Reviews
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3687655/
https://www.ncbi.nlm.nih.gov/pubmed/23489111
http://dx.doi.org/10.1111/bph.12166
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