Synthesis and structure-activity relationship of some 5-[[[(dialkylamino)alkyl]-1-piperidinyl]acetyl]-10,11-dihydro-5H-dibenzo[b,e][1,4]diazepin-11-ones as M2-selective antimuscarinics
作者:Victor I. Cohen、Jesse Baumgold、Biyun Jin、Rosanna De la Cruz、Waclaw J. Rzeszotarski、Richard C. Reba
DOI:10.1021/jm00053a021
日期:1993.1
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-
制备了一系列5-[[[[(二烷基氨基)烷基] -1-哌啶基]乙酰基] -10,11-二氢-5H-二苯并[b,e] [1,4]-二氮杂-11-酮M2选择性配体。评价化合物对毒蕈碱胆碱能受体的亲和力和选择性。研究的最好的M2选择性抗毒蕈碱剂是5-[[4- [4-二乙基氨基)丁基] -1-哌啶基]乙酰基] -10,11-二氢-5H-二苯并[b,e] [1,4]二氮杂ze -11-,在M2受体上的效力比以前已知的化合物(例如11-[[4- [4-(二乙基氨基)丁基] -1-哌啶基]乙酰基] -5,11-二氢-6H)强约10倍-吡啶基[2,3-b] [1,4]苯并二氮杂-1-酮(AQ-RA 741)。