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  • Title: Distinct agonist- and antagonist-binding sites on the glycine receptor.
    Author: Vandenberg RJ, Handford CA, Schofield PR.
    Journal: Neuron; 1992 Sep; 9(3):491-6. PubMed ID: 1326295.
    Abstract:
    The distinction between receptor-binding sites for agonists and antagonists underpins the pharmacological differences between these two classes of ligands. In the glycine receptor, antagonist (strychnine) binding requires an interaction with residues Lys-200 and Tyr-202. We now demonstrate that the agonist-binding site of this receptor is located at the residue Thr-204. The agonist-binding site interaction is thus likely to be mediated by hydrogen bonding and not by ionic interactions. Our results demonstrate that, in contrast to other studies of ligand-gated ion channel receptors, agonist- and antagonist-binding sites are composed of distinct amino acid residues.
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