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• W2412465862 endingPage "1043" @default.
• W2412465862 startingPage "1037" @default.
• W2412465862 abstract "The 5-hydroxytryptamine type 3 (5-HT₃) receptor is a transmitter-gated ion channel mediating neuronal excitation. The receptor native to neurons, or as a homopentameric assembly of 5-HT_3A receptor subunits, displays a species-dependent pharmacology exemplified by a 1800-fold difference in the potency of (+)-tubocurarine [(+)-Tc] as an antagonist of the current response mediated by mouse and human receptor orthologs. Here, we attempt to identify amino acid residues involved in binding (+)-Tc by use of chimeric and mutant 5-HT_3A subunits of mouse and human expressed in <i>Xenopus laevis</i> oocytes. Replacement of the entire extracellular N-terminal domain of the mouse 5-HT_3A(m5-HT_3A) subunit by that of the human ortholog and vice versa exchanged the differential potency of (+)-Tc, demonstrating the ligand binding site to be contained wholly within this region. Mutagenesis of multiple amino acid residues within a putative binding domain that exchanged nonconserved residues between mouse and human receptors shifted the apparent affinity of (+)-Tc in a reciprocal manner. The magnitude of the shift increased with the number of residues (3, 5, or 7) exchanged, with septuple mutations of m5-HT_3A and human 5-HT_3A subunits producing a 161-fold decrease and 53-fold increase in the apparent affinity of (+)-Tc, respectively. The effect of point mutations was generally modest, the exception being m5-HT_3A D206E, which produced a 9-fold decrease in apparent affinity. We conclude that multiple amino acids within a binding loop of human and mouse 5-HT_3Asubunits influence the potency of (+)-Tc." @default.
• W2412465862 created "2016-06-24" @default.
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• W2412465862 date "1999-06-01" @default.
• W2412465862 modified "2023-09-27" @default.
• W2412465862 title "Molecular Determinants of (+)-Tubocurarine Binding at Recombinant 5-Hydroxytryptamine_3AReceptor Subunits" @default.
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• W2412465862 doi "https://doi.org/10.1124/mol.55.6.1037" @default.
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