A new class of irreversible muscarinic antagonists: beta-haloethylamine furoates.
The synthesis of a class of ultra-long acting muscarinic antagonists is described. Furthermore, it is noted that the stability of the, in situ, aziridinium ion is sufficiently great so that these agents can be used to study the effect of temperature upon the conformation of the muscarinic cholinoceptor. The inactivation kinetics of these receptors as well as the dissociation constants, Kd, for all probes are presented.
D000818:Animals; D001388:Aziridines; D005021:Ethylamines / Q000138:chemical synthesis / Q000494:pharmacology; D006168:Guinea Pigs; D006868:Hydrolysis; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D007700:Kinetics; D009119:Muscle Contraction / Q000187:drug effects; D010276:Parasympatholytics; D011950:Receptors, Cholinergic / Q000187:drug effects; D013997:Time Factors
D001388:Aziridines; D005021:Ethylamines; D010276:Parasympatholytics; D011950:Receptors, Cholinergic