SB-277011 dihydrochloride

Description: SB-277011 dihydrochloride is a potent, selective, orally bioavailable and brain penetrate antagonist of dopamine D3 receptor(pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively). Target: Dopamine Receptor. Smiles: N#CC1=CC=C(C(CC2)=C1)CN2CC[C@@H](CC3)CC[C@H]3NC(C4=CC=NC5=C4C=CC=C5)=O.Cl.Cl. References: Stemp G, et al. Design and synthesis of trans-N-[4-[2-(6-cyano-1,2,3, 4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-4-quinolinecarboxamide (SB-277011): A potent and selective dopamine D(3) receptor antagonist with high oral bioavailability and CNS penetration in the rat. J Med Chem. 2000 May 4,43(9):1878-85.