Benzisoxazoles

Aromatic organic heterocyclic compounds that consist of benzene fused with an isoxazole; isoxazoles are an azole with an oxygen atom next to the nitrogen atom.

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Apexbio Technology LLC CGP 36216 hydrochloride 123691-29-2 10mg

CGP 36216 hydrochloride (CAS 123691-29-2) is a selective antagonist of the GABAB receptor exhibiting an IC50 of 43 M GABAB receptors are metabotropic G protein-coupled receptors expressed in both the central and peripheral nervous systems and are involved in modulating neuronal excitability and synaptic transmission In rat neocortical preparations CGP 36216 antagonizes baclofen-induced suppression of spontaneous discharges in a concentration-dependent manner but does not inhibit baclofen-mediated hyperpolarization at concentrations up to 1 mM Additionally CGP 36216 increases [3H]GABA release in electrically stimulated brain slices a response that can be reversed by baclofen indicating higher efficacy at presynaptic over postsynaptic GABAB receptors This compound is useful for studying GABAB receptor-mediated synaptic processes particularly presynaptic modulation