PG-01037 (hydrochloride)

PG-01037 is a selective dopamine D3 receptor antagonist (Kis = 0.7, 93, and 375 nM for HEK293 cells expressing human D3, D2, and D4 receptors, respectively). It inhibits quinpirole-induced stimulation of mitogenesis in CHO cells expressing human dopamine D3 receptors (EC50 = 3 nM). PG-01037 (32 mg/kg) reduces progressive-ratio methamphetamine self-administration in rats allowed extended access. It reduces loss of dopaminergic neurons in the substantia nigra pars compacta and improves motor performance in the coat-hanger test in a mouse model of Parkinson's disease induced by MPTP.Formal Name: N-[(2E)-4-[4-(2,3-dichlorophenyl)-1-piperazinyl]-2-buten-1-yl]-4-(2-pyridinyl)-benzamide, dihydrochloride. CAS Number: 675599-62-9. Molecular Formula: C26H26Cl2N4O . 2HCl. Formula Weight: 554.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/mL, DMSO: 30 mg/mL, Ethanol: 2 mg/mL. lambdamax: 254, 284 nm. SMILES: ClC1=CC=CC(N2CCN(C/C=C/CNC(C3=CC=C(C4=NC=CC=C4)C=C3)=O)CC2)=C1Cl.Cl.Cl. InChi Code: InChI=1S/C26H26Cl2N4O.2ClH/c27-22-6-5-8-24(25(22)28)32-18-16-31(17-19-32)15-4-3-14-30-26(33)21-11-9-20(10-12-21)23-7-1-2-13-29-23,,/h1-13H,14-19H2,(H,30,33),2*1H/b4-3+,,. InChi Key: DACFFMAXBWGOKQ-CZEFNJPISA-N.