MTS-Etomidate Selectively Reacts Within the GABAA Receptor Etomidate Binding Site

Identification of a GABAA receptor anesthetic binding site at subunit interfaces by photolabeling with an etomidate analog.

General anesthetics, including etomidate, act by binding to and enhancing the function of GABA type A receptors (GABA(A)Rs), which mediate inhibitory neurotransmission in the brain. Here, we used a radiolabeled, photoreactive etomidate analog ([(3)H]azietomidate), which retains anesthetic potency in vivo and enhances GABA(A)R function in vitro, to identify directly, for the first time, amino ac...

State-dependent etomidate occupancy of its allosteric agonist sites measured in a cysteine-substituted GABAA receptor.

A central axiom of ligand-receptor theory is that agonists bind more tightly to active than to inactive receptors. However, measuring agonist affinity in inactive receptors is confounded by concomitant activation. We identified a cysteine substituted mutant γ-aminobutyric acid type A (GABAA) receptor with unique characteristics allowing the determination of allosteric agonist site occupancy in ...

Etomidate as an antiarrhythmic.

Editor—We wish to report a case of etomidate reverting ventricular tachycardia to sinus rhythm. Although there have been several case reports and studies demonstrating the antiarrhythmic affects of propofol this has not been true of etomidate. A 59-yr-old man presented to the emergency department with a 2 h history of central chest pain radiating to the left arm and palpitations. He denied any ...

Etomidate as an antiarrhythmic

Editor—We wish to report a case of etomidate reverting ventricular tachycardia to sinus rhythm. Although there have been several case reports and studies demonstrating the antiarrhythmic affects of propofol this has not been true of etomidate. A 59-yr-old man presented to the emergency department with a 2 h history of central chest pain radiating to the left arm and palpitations. He denied any ...

Etomidate in Emergency Medicine