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CGP 13501 is a positive allosteric modulator of GABAB receptor [1].

The GABAB receptor is a metabotropic transmembrane receptors for GABA that is linked via G-protein to potassium channel. It stimulates the opening of K+ channel and hyperpolarize the neuron.

CGP 13501 is a positive allosteric modulator of GABAB receptor. In Chinese hamster ovary (CHO) cell line expressing GABAB(1b/2), CGP 13501 potentiated GABA-stimulated GTPγ[35S] binding to cell membranes [1]. In rat cortex, CGP13501 (10 μM) enhanced GABA-mediated activation of Gαo and increased GTPγ[35S] binding in the presence of GABA. Also, in the hippocampus and cerebellum, CGP13501 increased GABA-induced GTPγ[35S] binding and activation of Gαo. In rat cortex, hippocampus and cerebellum, CGP55845A blocked the influence of CGP13501 on GABA-induced GTPγ[35S] binding at Gαo with pIC50 values of 7.4, 7.31 and 6.82, respectively. In cells expressing GABAB(1b+2) receptors, CGP13501 increased GTPγ[35S] binding at Gαi1/3 [2].

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