Ontology highlight
ABSTRACT:
SUBMITTER: Berry CB
PROVIDER: S-EPMC4160761 | biostudies-literature | 2014 Sep
REPOSITORIES: biostudies-literature
Berry Cynthia B CB Bubser Michael M Jones Carrie K CK Hayes John P JP Wepy James A JA Locuson Charles W CW Daniels J Scott JS Lindsley Craig W CW Hopkins Corey R CR
ACS medicinal chemistry letters 20140709 9
Herein, we report the structure-activity relationship of a chiral morpholine-based scaffold, which led to the identification of a potent and selective dopamine 4 (D4) receptor antagonist. The 4-chlorobenzyl moiety was identified, and the compound was designated an MLPCN probe molecule, ML398. ML398 is potent against the D4 receptor with IC50 = 130 nM and K i = 36 nM and shows no activity against the other dopamine receptors tested (>20 μM against D1, D2S, D2L, D3, and D5). Further in vivo studie ...[more]