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Article

High Constitutive Activity Accounts for the Combination of Enhanced Direct Activation and Reduced Potentiation in Mutated GABAA Receptors.

Molecular pharmacology - 1 May 2018

Germann Allison L, Shin Daniel J, Kuhrau Christina R, Johnson Alexander D, Evers Alex S, Akk Gustav

Abstract excerpt

GABAA receptors activated by the transmitter GABA are potentiated by several allosterically acting drugs, including the intravenous anesthetic propofol. Propofol can also directly activate the receptor, albeit at higher concentrations. Previous functional studies have identified amino acid residues whose substitution reduces potentiation of GABA-activated receptors by propofol while enhancing the ability of...

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Identifiers

PMID: 29439087
DOI: 10.1124/mol.117.111435
PMCID: PMC5878668

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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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