文摘
Efficacy of bispyridine benzene mGlu5 negative allosteric modulators depends on molecule geometry. 1,4-disubstituted linear compounds have mGlu5 partial antagonist activity. 1,3-disubstituted angular compounds have mGlu5 full inverse agonist activity. 1,4- and 1,3-isomers bind preferentially to different receptor conformations according to computational docking.