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:
Reviews
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
Descripción
Sumario: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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