Competitive Interactions Between Propofol and Diazepam: Studies in GABA_A Receptors and Zebrafish.

ABSTRACT: Although propofol is among the most commonly administered general anesthetics, its mechanism of action is not fully understood. It has been hypothesized that propofol acts via a similar mechanism as (R)-ethyl 1-(1-phenylethyl)-1H-imidazole-5-carboxylate (etomidate) by binding within the GABA_A receptor transmembrane receptor domain at the two β ⁺/α ^- subunit interfaces with resultant positive allosteric modulation. To test this hypothesis, we leveraged the ability of diazepam to bind to those sites and act as a competitive antagonist. We used oocyte-expressed α ₁ β ₃ γ _2L GABA_A receptors to define the actions of diazepam (± flumazenil) on currents activated or potentiated by propo

SUBMITTER: Pence A 

PROVIDER: S-EPMC9667980 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature