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説明

CGP 7930 is a positive allosteric modulator of GABA_B receptors. It enhances GABA binding with a maximal effect of 143% compared to a GABA-only control in CHO cells membranes expressing the GABA_B(1b/2) receptor and enhances GABA binding to rat cortical membranes when used at a concentration of 30 μM. It is selective for GABA binding to heterodimeric GABA_B(1b/2) over monomeric GABA_B(1b) receptors. CGP 7930 potentiates the efficacy of the GABA_B receptor agonist baclofen in decreasing the spontaneous firing rate of dopaminergic neurons in the rat ventral tegmental area (VTA) in vitro (EC₅₀ = 0.27 μM). It also potentiates the sedative-reducing effects induced by the GABA_B receptor agonists baclofen and γ-hydroxybutyric acid (GHB) in rats when administered at doses ranging from 10 to 170 mg/kg, effects that can be blocked by the GABA_B receptor antagonist SCH 50911. CGP 7930 reduces self-administration of nicotine, alcohol, and cocaine in rodent models. It suppresses the acquisition of alcohol drinking behavior in alcohol-naïve Sardinian alcohol-preferring rats over a five-day period when administered at doses ranging from 25 to 100 mg/kg and transiently reduces the maintenance of alcohol drinking behavior in alcohol-experienced rats at a dose of 100 mg/kg.