Uses
AQ-RA 741 acts as a potent and highly specific muscarinic M2 receptor antagonist, with potential application towards the development of bronchodilator anti-muscarinic agents for humans.
Definition
ChEBI: 11-[2-[4-[4-(diethylamino)butyl]-1-piperidinyl]-1-oxoethyl]-5H-pyrido[2,3-b][1,4]benzodiazepin-6-one is a benzodiazepine.
Biological Activity
High affinity, selective muscarinic M 2 receptor antagonist (pK i values are 8.3, 7.7 and 6.82 for M 2 , M 1 and M 3 receptors, respectively). In vivo, displays cardioselectivity over intestinal, tracheal and bladder muscarinic receptors; inhibits vagally and agonist-induced bradycardia.
References
[1]. doods h, entzeroth m and mayer n. cardioselectivity of aq-ra 741, a novel tricyclic antimuscarinic drug. eur j pharmacol, 1991, 192(1):147-52.
[2]. gomeza j, shannon h, kostenis e, et al. pronounced pharmacologic deficits in m2 muscarinic acetylcholine receptor knockout mice. proc natl acad sci u s a, 1999, 96(4):1692-7.
