CGP 52432

CGP 52432 is an antagonist of GABAB receptors. It selectively reverses (-)-baclofen-induced inhibition of potassium-evoked GABA release over glutamate or somatostatin release (IC50s = 0.085, 3.35, and 9.26 µM, respectively) from rat cortical synaptosomes. CGP 52432 (10 µM) reduces paired-pulse inhibition of monosynaptic inhibitory potentials (IPSPs) by 80% in CA1 pyramidal neurons in rat hippocampal slices. It increases cell proliferation in the ventral subgranular zone of the dentate gyrus when administered at a dose of 3 mg/kg per day for 21 days and reduces immobility in the forced-swim test when administered at 10 mg/kg in stress-sensitive BALB/c mice. CGP 52432 (30 mg/kg) increases locomotor activity in mice. It also inhibits the analgesic effects of isovaline, GABA, and baclofen (Cay-18600) in a mouse model of hindpaw allodynia induced by prostaglandin E2 (PGE2, Cay-14010).Formal Name: P-[3-[[(3,4-dichlorophenyl)methyl]amino]propyl]-P-(diethoxymethyl)-phosphinic acid. CAS Number: 139667-74-6. Molecular Formula: C15H24Cl2NO4P. Formula Weight: 384.2. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. SMILES: ClC1=C(Cl)C=CC(CNCCCP(C(OCC)OCC)(O)=O)=C1. InChi Code: InChI=1S/C15H24Cl2NO4P/c1-3-21-15(22-4-2)23(19,20)9-5-8-18-11-12-6-7-13(16)14(17)10-12/h6-7,10,15,18H,3-5,8-9,11H2,1-2H3,(H,19,20). InChi Key: GJZVQXWEIYRHBE-UHFFFAOYSA-N.