The MCH1 receptor an anti-obesity target is allosterically inhibited by 8-methylquinoline derivatives possessing subnanomolar binding and long residence times

摘要

BACKGROUND AND PURPOSEMelanin-concentrating hormone receptor 1 (MCH1 receptor) antagonists are being considered as anti-obesity agents. The present study reports a new class of MCH1 receptor antagonists with an 8-methylquinoline scaffold. The molecular mechanism of MCH1 receptor blockade by these antagonists was examined.