Abstract
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 non-competitive antagonists identified with this ability has increased in recent years. In this review, we discuss the differences between 5-HT₃A and 5-HT₃AB receptors and describe the possible sites of action of compounds that can distinguish between them.
© 2013 The Authors. British Journal of Pharmacology © 2013 The British Pharmacological Society.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Allosteric Regulation / drug effects
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Animals
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Antiemetics / chemistry
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Antiemetics / metabolism
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Antiemetics / pharmacology
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Antiemetics / therapeutic use
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Binding Sites / drug effects
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Binding, Competitive / drug effects
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Drug Partial Agonism
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Humans
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Ligands
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Models, Molecular*
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Molecular Conformation
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Protein Multimerization
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Protein Subunits / antagonists & inhibitors
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Protein Subunits / chemistry
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Protein Subunits / genetics
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Protein Subunits / metabolism
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Receptors, Serotonin, 5-HT3 / chemistry
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Receptors, Serotonin, 5-HT3 / genetics
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Receptors, Serotonin, 5-HT3 / metabolism*
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Recombinant Proteins / chemistry
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Recombinant Proteins / metabolism
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Serotonin 5-HT3 Receptor Agonists / chemistry
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Serotonin 5-HT3 Receptor Agonists / metabolism
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Serotonin 5-HT3 Receptor Agonists / pharmacology
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Serotonin 5-HT3 Receptor Agonists / therapeutic use
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Serotonin 5-HT3 Receptor Antagonists / chemistry
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Serotonin 5-HT3 Receptor Antagonists / metabolism
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Serotonin 5-HT3 Receptor Antagonists / pharmacology
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Serotonin 5-HT3 Receptor Antagonists / therapeutic use
Substances
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Antiemetics
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HTR3A protein, human
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HTR3B protein, human
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Ligands
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Protein Subunits
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Receptors, Serotonin, 5-HT3
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Recombinant Proteins
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Serotonin 5-HT3 Receptor Agonists
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Serotonin 5-HT3 Receptor Antagonists