title: Discriminating between 5-HT₃A and 5-HT₃AB receptors.
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.
authors.affiliation: Department of Biochemistry, University of Cambridge, Cambridge, UK. ajt44@cam.ac.uk
authors.forename: A J
authors.initials: AJ
authors.lastname: Thompson
authors.forename: S C R
authors.initials: SC
authors.lastname: Lummis
mesh_terms: D000494:Allosteric Regulation / Q000187:drug effects; D000818:Animals; D000932:Antiemetics / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D001665:Binding Sites / Q000187:drug effects; D001667:Binding, Competitive / Q000187:drug effects; D054333:Drug Partial Agonism; D006801:Humans; D008024:Ligands; D008958:Models, Molecular; D008968:Molecular Conformation; D055503:Protein Multimerization; D021122:Protein Subunits / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000235:genetics / Q000378:metabolism; D044406:Receptors, Serotonin, 5-HT3 / Q000737:chemistry / Q000235:genetics / Q000378:metabolism*; D011994:Recombinant Proteins / Q000737:chemistry / Q000378:metabolism; D058827:Serotonin 5-HT3 Receptor Agonists / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D058831:Serotonin 5-HT3 Receptor Antagonists / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D000932:Antiemetics; C509409:HTR3A protein, human; C509410:HTR3B protein, human; D008024:Ligands; D021122:Protein Subunits; D044406:Receptors, Serotonin, 5-HT3; D011994:Recombinant Proteins; D058827:Serotonin 5-HT3 Receptor Agonists; D058831:Serotonin 5-HT3 Receptor Antagonists