Propofol

Matt Jones jonesmat at ohsu.edu
Fri Oct 11 11:33:56 EST 1996


In article <malbert-1010961718130001 at malbert.rennes.inra.fr> Charles
Henri Malbert, malbert at st-gilles.rennes.inra.fr writes:
>Hello,
>We are looking for the receptor type on which propofol is binding to and
>(ultimately) act through.
>Thanks in advance

Hi,

Propofol can interact,  as can most small hydrophobic molecules, with a
lot of receptors. Assuming that you're interested in the actions relevant
to producing anesthesia, the important criteria is which receptors are
affected at clinically relevant concentrations (anywhere from 10-50 !M,
probably). The best evidence demonstrates dramatic actions at GABA-A
channels at these concentrations, although effects on voltage-gated
calcium channels, nicotinic receptors, 5HT-3 receptors, calcium handling
systems and potassium channels have also been reported. Of all these, the
GABA-A receptor is the most commonly affected target of general
anesthetics at relevant concentrations. Propofol both potentiates the
channel response to GABA, and directly activates the channel in the
absence of GABA:

Hales and Lambert (1991) The actions of propofol on inhibitory amino acid
receptors of bovine adrenomedullary chromaffin cells and rodent central
neurons. Br. J. Pharmacol. 104, 619-628.

Hara et al. (1993) Propofol activates GABA-A receptor-chloride ionophore
complex in dissociated hippocampal pyramidal neurons of the rat.
Anesthesiology 79, 781-788.

Orser et al. (1994) Propofol modulates activation and desensitization of
GABA-A receptors in cultured murine hippocampal neurons. J. Neurosci. 14,
7747-7760.

Cheers,
Matt



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