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Article

State-dependent etomidate occupancy of its allosteric agonist sites measured in a cysteine-substituted GABAA receptor.

Molecular pharmacology - 1 Jun 2013

Stewart Deirdre S, Hotta Mayo, Desai Rooma, Forman Stuart A

Abstract excerpt

A central axiom of ligand-receptor theory is that agonists bind more tightly to active than to inactive receptors. However, measuring agonist affinity in inactive receptors is confounded by concomitant activation. We identified a cysteine substituted mutant γ-aminobutyric acid type A (GABAA) receptor with unique characteristics allowing the determination of allosteric agonist site occupancy in both inactive and...

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Identifiers

PMID: 23525330
DOI: 10.1124/mol.112.084558
PMCID: PMC3657098

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 6 Sept 2026. Manifest publication-graph-cohort-2026-09-06.1.

Source receipt: pubmed, retrieved 6 Sept 2026.

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