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Article

Three arginines in the GABAA receptor binding pocket have distinct roles in the formation and stability of agonist- versus antagonist-bound complexes.

Molecular pharmacology - 1 Oct 2011

Goldschen-Ohm Marcel P, Wagner David A, Jones Mathew V

Abstract excerpt

Binding of the agonist GABA to the GABA(A) receptor causes channel gating, whereas competitive antagonists that bind at the same site do not. The details of ligand binding are not well understood, including which residues interact directly with ligands, maintain the structure of the binding pocket, or transduce the action of binding into opening of the ion channel gate. Recent work suggests that the amine group...

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PMID: 21764985
DOI: 10.1124/mol.111.072033
PMCID: PMC3187534

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