title: On the pharmacology of Org 6338 (2beta, 16beta-dipiperidino - 5alpha - androstan - 3alpha - ol acetate dimethobromide), a new steroidal neuromuscular blocking agent.
abstract: Org 6368 is a homologue of pancuronium bromide. Its interactions with other agents in the cat sciatic nerve-gastrocnemius muscle preparation revealed that paralysis was of the non-depolarizing type. This was confirmed in experiments using avian muscle. Org 6368 is a potent muscle relaxant being 2-4 times as potent as (+)-tubocurarine in the cat. Paralysis in the cat is rapid in onset and of appreciably shorter duration than that of pancuronium and (+)-tubocurarine. Repeated injections of the same dose of Org 6368 show no cumulative effect. Muscle relaxant doses generally cause a slight increase in both blood pressure and heart rate. Although its histamine-releasing capacity is greater than that of pancuronium it is less than that of (+)-tubocurarine. Org 6368 shares with pancuronium a very weak effect on both the muscarinic receptor and ganglionic transmission. Differences in the muscle relaxant profiles of Org 6368 and pancuronium are discussed.
mesh_terms: D000818:Animals; D001339:Autonomic Fibers, Preganglionic / Q000502:physiology; D002415:Cats; D002645:Chickens; D004558:Electric Stimulation; D005260:Female; D005703:Gallamine Triethiodide / Q000494:pharmacology; D005727:Ganglia, Spinal / Q000187:drug effects; D006168:Guinea Pigs; D006584:Hexamethonium Compounds / Q000494:pharmacology; D006636:Histamine Release / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D009132:Muscles / Q000187:drug effects; D009466:Neuromuscular Blocking Agents / Q000494:pharmacology*; D009469:Neuromuscular Junction / Q000187:drug effects; D010197:Pancuronium / Q000031:analogs & derivatives* / Q000494:pharmacology; D010276:Parasympatholytics / Q000494:pharmacology; D010791:Phrenic Nerve / Q000502:physiology; D012584:Sciatic Nerve / Q000502:physiology; D009435:Synaptic Transmission / Q000187:drug effects; D014403:Tubocurarine / Q000494:pharmacology
chemical_list: D006584:Hexamethonium Compounds; D009466:Neuromuscular Blocking Agents; D010276:Parasympatholytics; C011142:Org 6368; D010197:Pancuronium; D005703:Gallamine Triethiodide; D014403:Tubocurarine