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The Anaesthetic Agent Propofol Interacts With GABA(B)-receptors: An Electrophysiological Study in Rat

The Anaesthetic Agent Propofol Interacts With GABA(B)-receptors: An Electrophysiological Study in Rat

L Schwieler, D S Delbro, G Engberg, S Erhardt

Life Sci. 2003 May 2;72(24):2793-801.

PMID: 12679195

Abstract:

The mode of action by which propofol induces anaesthesia is not fully understood, although several studies suggest that the compound acts via potentiation of brain GABA(A)-receptors. The aim of the present study is to investigate a putative GABA(B)-receptor agonistic action of propofol. For this purpose the action of propofol on a GABA-receptor mediated regulation of dopamine neurons was analyzed with extracellular single unit recordings of dopaminergic neurons of the substantia nigra in chloral hydrate anaesthetized rats. Intravenous administration of propofol (1-16 mg/kg) was found to dose-dependently decrease the firing rate and burst firing activity of nigral DA neurons. These effects by propofol were effectively antagonized by pretreatment with the selective GABA(B)-receptor antagonist CGP 35348 (200 mg/kg, i.v.) but not by pretreatment with the GABA(A)-receptor antagonist picrotoxin (4.5 mg/kg, i.v.). It is proposed that an activation of central GABA(B)-receptors may, at least partially, contribute to the anesthetic properties of propofol.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
ALP123690799	CGP 35348 hydrate		123690-79-9 (free acid)	Price

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