A newly developed anesthetic based on a unique chemical core.

ABSTRACT: Intravenous anesthetic agents are associated with cardiovascular instability and poorly tolerated in patients with cardiovascular disease, trauma, or acute systemic illness. We hypothesized that a new class of intravenous (IV) anesthetic molecules that is highly selective for the slow type of γ-aminobutyric acid type A receptor (GABA_AR) could have potent anesthetic efficacy with limited cardiovascular effects. Through in silico screening using our GABA_AR model, we identified a class of lead compounds that are N-arylpyrrole derivatives. Electrophysiological analyses using both an in vitro expression system and intact rodent hippocampal brain slice recordings demonstrate a GABA_AR-mediated mechanism. In vivo experiments also demonstrate overt anesthetic

SUBMITTER: Cayla NS 

PROVIDER: S-EPMC6681746 | biostudies-literature | 2019 Jul

REPOSITORIES: biostudies-literature