[Binding of dicyclohexylamide derivatives of N-substituted aminocarboxylic acids with muscarinic cholinoreceptors and beta-adrenoreceptors]. / Sviazyvanie proizvodnykh ditsiklogeksilamidov N-zameshchennykh aminokarbonovykh kislot s muskarinovymi kholinoretseptorami i beta-adrenoretseptorami.

ABSTRACT

The binding of N-substituted aminocarboxylic acid dicyclohexylamide (NACA-DCHA) derivatives to M-1 muscarinic cholinoreceptors (MRs) in rat brain cortex and and beta-1 adrenoreceptors (ARs) in rat heart was studied. The maximum MR affinity was observed for AL-275 (IC50, 2.8 microM) and AL-315 (IC 50, 3.2 microM) preparations. The other compounds (except AL-310 with IC50 > 100 microM) interacted with MR at a lower affinity. The binding to beta-1 AR in rat heart was observed for a single preparation AL-298 (IC50, 38 microM). The antimuscarinic activity of some NACA-DCHA derivatives, especially AL-275 and AL-315) may play a significant role in realization of the antiarrhythmic activity.