Document Report Card

ID: ALA1143627

Journal: J Med Chem

Title: Enantiomerically pure hexahydropyrazinoquinolines as potent and selective dopamine 3 subtype receptor ligands.

Authors: Ding K, Ding K, Chen J, Ji M, Wu X, Varady J, Yang CY, Lu Y, Deschamps JR, Levant B, Wang S.

Abstract: We report the design and synthesis of a series of enantiomerically pure hexahydropyrazinoquinolines as potent and selective ligands for the dopamine 3 subtype receptor using a newly developed synthetic method and using in vitro pharmacological evaluation. Our efforts yielded optically pure ligands with high affinities for the D(3) receptor and outstanding selectivity over closely related D(1)-like and D(2)-like receptors. For example, compound 38a has a K(i) value of 5.7 nM to the D(3) receptor and selectivity greater than 10000- and 1600-fold over the D(1)-like and D(2)-like receptors, respectively, and thus is one of the most selective D(3) ligands reported to date.

CiteXplore: 15857123

DOI: 10.1021/jm049031l