E161111 is an ultra-short-acting etomidate analogue with stable haemodynamics that elicits only slight adrenocortical suppression in rats.

ABSTRACT:

Purpose

We report on a novel ultra-short-acting etomidate analogue, E161111, which has the same primary metabolite as etomidate.

Methods

The metabolic rate of E161111 was determined in rat plasma and liver homogenate. Rats were infused for 30 or 60 min to maintain light sedation at Richmond Agitation-Sedation Scale (RASS) for -2 to 0 score. Mean arterial pressure (MAP) was monitored during 30 min infusion. The serum corticosterone was determined during and 3 h after infusion as a measure of adrenocortical function.

Results

E161111 was not detected in rat plasma at 1 min (t_1/2 = 6.69 ± 0.07 s) and in rat liver homogenates at 5 min (t_1/2 = 10.20 ± 3.76 s); its main metabolic product was etomidate acid. The recovery time from loss of righting reflex

SUBMITTER: Wang B 

PROVIDER: S-EPMC9138173 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature