Chemical Name:(R)-1-(1-Phenylethyl)-1H-imidazole-5-carboxylic acid
ethyl ester
Biological Activity:
General
anaesthetic with GABA modulatory and GABA-mimetic actions; selectively
interacts with β2- and β3-subunit containing GABAA
receptors. Short acting and potent hypnotic, with low toxicity.
Gieseet al (1983) Etomidate: a new
intravenous anesthetic induction agent. Pharmacother. 3 251. Belelli
et al (1997) The interaction of the general anesthetic etomidate
with the γ-aminobutyric
acid type A receptor is influenced by a single amino acid.
Proc.Natl.Acad.Sci.USA 94 11031. Moodyet al (1998)
Distinct structural requirements for the direct and indirect actions of the
anaesthetic etomidate at GABAA receptors. Toxicol.Lett. 100-101
209.
Selective antagonist of neuro-steroid potentiation and direct gating of GABAA receptors. Selectively reduces the effects of 5α-reduced steroids compared to 5β-reduced steroids & displays no effect on potentiation evoked by barbiturates & benzodiazepines. Attenuates 3α,5α-THP-induced loss of righting reflex and total sleep time following i.c.v administration in rats.