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CGP 36742 is an antagonist of GABAB receptors (IC50 = 36 µM).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
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1. The actions of orally active GABAB receptor antagonists on GABAergic transmission in vivo and in vitro. Eur. J. Pharmacol. 233(2-3), 179-186 (1993).
2. CGP 36742: The first orally active GABAB blocker improves the cognitive performance of mice, rats, and rhesus monkeys. Behav. Neural Biol. 60(1), 62-68 (1993).
3. Antidepressant-