title: Anionic cyclophanes as potential reversal agents of muscle relaxants by chemical chelation.
abstract: A series of carboxyl-containing cyclophanes have been designed and synthesised as chemical chelators (or host molecules) of cationic muscle relaxant drugs (or guest molecules). Three of these cyclophane derivatives, 1-3, have been shown by NMR to form 1:1 complexes with the muscle relaxants pancuronium, and gallamine, in D(2)O, with association constants up to 10(4) M(-1). When tested in an in vitro chick biventer muscle preparation, the cyclophanes reversed the neuromuscular block induced by pancuronium and gallamine, with having the most effective reversal against pancuronium (EC(50) 40 microM.
authors.affiliation: Department of Analytical Chemistry, Organon Laboratories Ltd., Newhouse, Lanarkshire ML1 5SH, Scotland, UK.
authors.forename: Kenneth S
authors.initials: KS
authors.lastname: Cameron
authors.forename: Lee
authors.initials: L
authors.lastname: Fielding
authors.forename: Rona
authors.initials: R
authors.lastname: Mason
authors.forename: Alan W
authors.initials: AW
authors.lastname: Muir
authors.forename: David C
authors.initials: DC
authors.lastname: Rees
authors.forename: Simon
authors.initials: S
authors.lastname: Thorn
authors.forename: Ming Qiang
authors.initials: MQ
authors.lastname: Zhang
mesh_terms: D000818:Animals; D000838:Anions / Q000737:chemistry; D002614:Chelating Agents / Q000494:pharmacology*; D002645:Chickens; D004988:Ethers, Cyclic / Q000494:pharmacology*; D005703:Gallamine Triethiodide / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D009465:Neuromuscular Agents / Q000494:pharmacology*; D009469:Neuromuscular Junction / Q000187:drug effects* / Q000502:physiology; D003473:Neuromuscular Nondepolarizing Agents / Q000494:pharmacology; D010197:Pancuronium / Q000494:pharmacology
chemical_list: D000838:Anions; D002614:Chelating Agents; D004988:Ethers, Cyclic; D009465:Neuromuscular Agents; D003473:Neuromuscular Nondepolarizing Agents; D010197:Pancuronium; D005703:Gallamine Triethiodide