1 results match your criteria: "Harvard Medical School (S.S.J.[Affiliation]"
Competitive Antagonism of Etomidate Action by Diazepam: In Vitro GABAA Receptor and In Vivo Zebrafish Studies.
Anesthesiology
September 2020
From the Department of Anesthesia, Critical Care, and Pain Medicine, Massachusetts General Hospital (M.M., H.H., A.P., X.Z., S.A.F., K.W.M., D.E.R.) Department of Neurobiology, Harvard Medical School (S.S.J., J.B.C.), Boston, Massachusetts.
Background: Recent cryo-electron microscopic imaging studies have shown that in addition to binding to the classical extracellular benzodiazepine binding site of the α1β3γ2L γ-aminobutyric acid type A (GABAA) receptor, diazepam also binds to etomidate binding sites located in the transmembrane receptor domain. Because such binding is characterized by low modulatory efficacy, the authors hypothesized that diazepam would act in vitro and in vivo as a competitive etomidate antagonist.
Methods: The concentration-dependent actions of diazepam on 20 µM etomidate-activated and 6 µM GABA-activated currents were defined (in the absence and presence of flumazenil) in oocyte-expressed α1β3γ2L GABAA receptors using voltage clamp electrophysiology.