Approaches to short-acting neuromuscular blocking agents: nonsymmetrical bis-tetrahydroisoquinolinium mono- and diesters.
Nonsymmetrical bisquaternary mono- and diesters combining the potency-enhancing properties of the (1R)-laudanosinium group with a second unhindered quaternary ammonium moiety have been studied as a means of promoting short action with high-potency neuromuscular block. Atracurium-related nonsymmetrical diesters showed high potency, freedom from vagal blockade at neuromuscular blocking doses, and short action. Nonsymmetrical monoesters were short acting but showed varying degrees of vagal block.
Dhar
N C
NC
Department of Pharmaceutical Sciences, University of Strathclyde, Glasgow, Scotland.
Maehr
R B
RB
Masterson
L A
LA
Midgley
J M
JM
Stenlake
J B
JB
Wastila
W B
WB
D000818:Animals; D002415:Cats; D002855:Chromatography, Thin Layer; D004952:Esters; D006868:Hydrolysis; D007546:Isoquinolines / Q000737:chemistry / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D009466:Neuromuscular Blocking Agents / Q000737:chemistry / Q000494:pharmacology*; D011806:Quinolinium Compounds / Q000737:chemistry / Q000494:pharmacology*; D014630:Vagus Nerve / Q000187:drug effects
D004952:Esters; D007546:Isoquinolines; D009466:Neuromuscular Blocking Agents; D011806:Quinolinium Compounds; C001522:laudanosine