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“Background:Most anesthetics, particularly intravenous agents such as propofol and etomidate, enhance the actions of the neurotransmitter & ggr;-aminobutyric acid (GABA) at the GABA type A receptor.”
“However, current theories on how propofol enhances the inhibitory effects of gamma-aminobutyric acid (GABA) cannot fully explain its protective action on the brain.”
“ Propofol and some barbiturates also decrease the rate and extent of desensitization as indicated by a prolongation in the decay of currents evoked by saturating concentrations of GABA.”
“4 With the appropriate agonist EC10, propofol enhanced GABA and glycine‐evoked currents to approximately the maximal response produced by a saturating concentration of either agonist (i.e. Imax).”
British journal of pharmacology • 1997 | View Paper
“ Propofol also potentiated alpha 4 beta 1 gamma 2 GABA responses but to a level more comparable to that of alpha 1 beta 1 gamma 2, suggesting that these compounds act via different sites.”
“ Propofol acts as a positive allosteric modulator of γ-aminobutyric acid type A receptors (GABAARs), an interaction necessary for its anesthetic potency in vivo as a general anesthetic.”
The Journal of Biological Chemistry • 2014 | View Paper
“The action of propofol on GABA and glutamate, neurotransmitters critical for influencing level of arousal and consciousness, probably accounts for its anesthetic properties and potential for lethal overdose.”
“Increasing GABA efficacy on alpha4/6beta3delta and alpha4beta3 receptors is likely to make an important contribution to the anesthetic effects of etomidate, propofol and the neurosteroid THDOC.”
“Indeed, although propofol had significant effects on GABA potency in wild-type receptors, we found that propofol produced no corresponding increase in GABA efficacy.”