Competitive Antagonism of Etomidate Action by Diazepam In Vitro GABA A Receptor and In Vivo Zebrafish Studies

ConclusionsAt micromolar concentrations and in the presence of flumazenil to inhibit allosteric modulationvia the classical benzodiazepine binding site of the GABAA receptor, diazepam acts as anin vitro andin vivo competitive etomidate antagonist.Editor ’s PerspectiveWhat We Already Know about This TopicDiazepam binds to the γ-aminobutyric acid type A (GABAA) receptor high-affinity extracellular benzodiazepine siteDiazepam can also bind to the GABAA receptor transmembrane etomidate siteIt is unknown whether diazepam or similar compounds can antagonize etomidateWhat This Article Tells Us That Is NewIn vitro andin vivo zebrafish studies show that diazepam and other like compounds can competitively antagonize etomidate at the GABAA receptor etomidate binding siteThis provides proof-of-concept for development of competitive anesthetic antagonists
Source: Anesthesiology - Category: Anesthesiology Source Type: research