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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...
Autores principales: | , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Blackwell Publishing Ltd
2013
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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. |
format | Online Article Text |
id | pubmed-3687655 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2013 |
publisher | Blackwell Publishing Ltd |
record_format | MEDLINE/PubMed |
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 |
work_keys_str_mv | AT thompsonaj discriminatingbetween5ht3aand5ht3abreceptors AT lummisscr discriminatingbetween5ht3aand5ht3abreceptors |