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The use of the unsaturated peptide, glycyldehydrophenylalanine, as the substrate for aminopeptidase in the isolation procedure provided a facile assay making possible the analysis of a large number of fractions in a relatively short period of time. Expand
Restoration of soman-blocked neuromuscular transmission in human and rat muscle by the bispyridinium non-oxime MB327 in vitro.
The ability of MB327 to counteract soman-impaired neuromuscular transmission was investigated in human intercostal muscle and rat diaphragm preparations and the therapeutic effect of MB 327 could be washed out, indicating a direct effect at the nicotinic receptor level. Expand
Protection against nerve agent poisoning by a noncompetitive nicotinic antagonist.
This study demonstrates that the compound 1,1'-(propane-1,3-diyl)bis(4-tert-butylpyridinium), which blocks open nicotinic ion channels noncompetitively, is able to reverse the neuromuscular paralysis after nerve agent poisoning in vitro and to protect guinea pigs against poisoning by nerve agents when used as part of a therapeutic drug combination including a muscarinic antagonist. Expand
Interaction of bispyridinium compounds with the orthosteric binding site of human α7 and Torpedo californica nicotinic acetylcholine receptors (nAChRs).
The results of the present study do not indicate a correlation between the affinity to the orthosteric binding site and the functional improvement of neuromuscular transmission and it is assumed that other mechanisms contribute to the therapeutic effect of the tested compounds. Expand
1,1′-(Propane-1,3-diyl)bis(4-tert-butylpyridinium) di(methanesulfonate) protects guinea pigs from soman poisoning when used as part of a combined therapy
Syntheses of 1,1-(propane-1,3-diyl)bis(4-tert-butylpyridinium) diiodide (MB327) and its di(methanesulfonate) salt (MB399) are described. Protection experiments in guinea-pigs showed that MB399, aExpand
Pharmacokinetic profile and quantitation of protection against soman poisoning by the antinicotinic compound MB327 in the guinea-pig.
MB327 or related compounds may be of utility in treatment of nerve agent poisoning as a component of therapy with atropine, anticonvulsant and oxime, or alternatively as an infusion under medical supervision. Expand
Affinities of bispyridinium non-oxime compounds to [(3)H]epibatidine binding sites of Torpedo californica nicotinic acetylcholine receptors depend on linker length.
A homologous series of unsubstituting and 4-tert-butyl-substituted bispyridinium compounds with different alkane linker lengths was investigated in competition binding experiments and it was demonstrated that divalent cations increased the affinity of [(3)H]epibatidine. Expand
Bispyridinium Compounds Inhibit Both Muscle and Neuronal Nicotinic Acetylcholine Receptors in Human Cell Lines
It is demonstrated that bispyridinium compounds inhibit both neuronal and muscle nicotinic receptors and that their potency depends on the length of the hydrocarbon chain linking the two pyrid inium moieties. Expand
Fluorinated pyridine derivatives: Part 1. The synthesis of some mono- and bis-quaternary pyridine salts of potential use in the treatment of nerve agent poisoning
Abstract Experiments were performed to determine whether F- and CF 3 -substituted pyridines undergo quaternization with iodomethane (1:1 molar ratio in THF) and 1,3-diiodopropane (2:1 molar ratio inExpand
Competition radioligand binding assays for the investigation of bispyridinium compound affinities to the human muscarinic acetylcholine receptor subtype 5 (hM(5) ).
Standard treatment of poisoning by organophosphorus (OP) nerve agents with atropine and oximes lacks efficacy with some nerve agents. Promising in vitro and in vivo results were obtained with theExpand