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Engineered Flumazenil Recognition Site Provides Mechanistic Insight Governing Benzodiazepine Modulation in GABAA Receptors.

ACS chemical biology - 17 Aug 2018

Siebert David C B, Bampali Konstantina, Puthenkalam Roshan, Varagic Zdravko, Sarto-Jackson Isabella, Scholze Petra, Sieghart Werner, Mihovilovic Marko D, Schnürch Michael, Ernst Margot

Abstract excerpt

The anxiolytic, anticonvulsant, muscle-relaxant, and sedative-hypnotic effects of benzodiazepine site ligands are mainly elicited by allosteric modulation of GABAA receptors via their extracellular αx+/γ2- ( x = 1, 2, 3, 5) interfaces. In addition, a low affinity binding site at the homologous α+/β- interfaces was reported for some benzodiazepine site ligands. Classical benzodiazepines and pyrazoloquinolinones...

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PMID: 29989390
DOI: 10.1021/acschembio.8b00145

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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