Etomidate and Etomidate Analog Binding and Positive Modulation of γ-Aminobutyric Acid Type A Receptors Evidence for a State-dependent Cutoff Effect

Conclusions Steric hindrance selectively reduces phenyl ring –substituted etomidate analog binding affinity to the two β+− α– anesthetic binding sites on the GABAA receptor ’s open state, suggesting that the binding pocket where etomidate’s phenyl ring lies becomes smaller as the receptor isomerizes from closed to open.
Source: Anesthesiology - Category: Anesthesiology Source Type: research