[Binding of dicyclohexylamide derivatives of N-substituted aminocarboxylic acids with muscarinic cholinoreceptors and beta-adrenoreceptors].
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.
Brusova
E G
EG
Laboratory of Circulation System Pharmacology, Institute of Pharmacology, Russian Academy of Medical Sciences, Baltiiskaya ul. 8, Moscow, 125315 Russia.
Kaverina
N V
NV
Likhosherstov
A M
AM
D000596:Amino Acids / Q000378:metabolism*; D000818:Animals; D001921:Brain / Q000378:metabolism; D002264:Carboxylic Acids / Q000378:metabolism; D002462:Cell Membrane / Q000378:metabolism; D003514:Cyclohexylamines / Q000378:metabolism*; D009206:Myocardium / Q000378:metabolism; D051381:Rats; D011943:Receptors, Adrenergic, beta / Q000378:metabolism*; D011976:Receptors, Muscarinic / Q000378:metabolism*; D013329:Structure-Activity Relationship
D000596:Amino Acids; D002264:Carboxylic Acids; D003514:Cyclohexylamines; D011943:Receptors, Adrenergic, beta; D011976:Receptors, Muscarinic