A GABAB receptor antagonist
CGP 36742 is an antagonist of GABAB receptors (IC50 = 36 ?M).1 It is selective for GABAB over a panel of 11 receptors, including GABAA, at 1 mM. CGP 36742 (3 mg/kg) reduces paired-pulse inhibition of the late inhibitory postsynaptic potential (IPSP) in CA1 pyramidal neurons in rats. It increases latency to step-down in a passive avoidance test in mice in a dose-dependent manner.2 CGP 36742 (10 and 30 mg/kg) decreases immobility time in the forced swim test in mice.3
1.Olpe, H.R., Steinmann, M.W., Ferrat, T., et al.The actions of orally active GABAB receptor antagonists on GABAergic transmission in vivo and in vitroEur. J. Pharmacol.233(2-3)179-186(1993) 2.Mondadori, C., Jaekel, J., and Preiswerk, G.CGP 36742: The first orally active GABAB blocker improves the cognitive performance of mice, rats, and rhesus monkeysBehav. Neural Biol.60(1)62-68(1993) 3.Nowak, G., Partyka, A., Palucha, A., et al.Antidepressant-like activity of CGP 36742 and CGP 51176, selective GABAB receptor antagonists, in rodentsBr. J. Pharmacol.149(5)581-590(2006)
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