CGP 36742

A GABAB receptor antagonist

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库存: 现货

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5mg

￥1300.00

1040.00

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10mg

￥2337.00

1870.00

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25mg

￥4312.00

3450.00

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50mg

￥7337.00

5870.00

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Background

CGP 36742 is an antagonist of GABA_B receptors (IC₅₀ = 36 ?M).¹ It is selective for GABA_B over a panel of 11 receptors, including GABA_A, 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)