In search of new neuromuscular blocking drugs with quick onset and short duration of effect.
In experiments using cats the neuromuscular blocking effect of bis-trimethylammonium derivatives having a non-depolarizing mode of action had an onset of action shorter than that of their triethylammonium analogs. The difference in equieffective doses of neuromuscular blocking agents administered intravenously or intraarterially was less in the case of compounds with rigid molecules than that with flexible molecules. Results indicate that a more considerable portion of flexible substance absorbs on the 'site of loss' in blood vessels than for rigid compounds. This suggests that rigid molecules promote a faster achievement of effective concentration of a neuromuscular blocking agent at synapses. Proceeding from these data a bis-trimethylammonium derivative with a rigid molecule, IEM-1213, was synthesized and studied in cats.
Danilov
A F
AF
Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, St.-Petersburg.
Gmiro
V E
VE
Fedorov
D J
DJ
D000818:Animals; D008725:Bis-Trimethylammonium Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002415:Cats; D005260:Female; D007269:Injections, Intra-Arterial; D007275:Injections, Intravenous; D008297:Male; D009126:Muscle Relaxation / Q000187:drug effects; D009132:Muscles / Q000187:drug effects*; D003473:Neuromuscular Nondepolarizing Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*
D008725:Bis-Trimethylammonium Compounds; C089301:IEM 1213; D003473:Neuromuscular Nondepolarizing Agents