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Discriminating between 5-HT?A and 5-HT?AB receptors.


ABSTRACT: The 5-HT3B subunit was first cloned in 1999, and co-expression with the 5-HT3A subunit results in heteromeric 5-HT?AB receptors that are functionally distinct from homomeric 5-HT?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?A from 5-HT?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?A and 5-HT?AB receptors and describe the possible sites of action of compounds that can distinguish between them.

SUBMITTER: Thompson AJ 

PROVIDER: S-EPMC3687655 | biostudies-literature | 2013 Jun

REPOSITORIES: biostudies-literature

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Discriminating between 5-HT₃A and 5-HT₃AB receptors.

Thompson A J AJ   Lummis S C R SC  

British journal of pharmacology 20130601 4


The 5-HT3B subunit was first cloned in 1999, and co-expression with the 5-HT3A subunit results in heteromeric 5-HT₃AB receptors that are functionally distinct from homomeric 5-HT₃A 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-HT₃A from 5-HT₃AB receptors has recently been described, and the number of n  ...[more]

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