Synthesis and structure-activity relationship of some 5- [[[(dialkylamino)alkyl]-1-piperidinyl]acetyl]-10,11-dihydro-5H- benzo[b,e][1,4]diazepin-11-ones as M2-selective antimuscarinics

Article abstract of DOI:10.1021/jm00053a021

A series of 5-[[[(dialkylamino)alkyl]-1-piperidinyl]acetyl]-10,11-dihydro- 5H-dibenzo[b,e][1,4]-diazepin-11-ones were prepared as potential M₂- selective ligands. The compounds were evaluated for their affinity and selectivity for the muscarinic cholinergic receptor. The best M₂-selective antimuscarinic agent studied is 5-[[4-[4-(diethylamino)butyl]-1- piperidinyl]acetyl]-10,11-dihydro-5H-dibenzo[b,e][1,4]diazepin-11-one, which is approximately 10 times more potent at M₂ receptors than previously known compounds such as 11-[[4-[4-(diethylamino)butyl]-1-piperidinyl]acetyl]-5,11- dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one (AQ-RA 741).