Add time:08/20/2019         Source:sciencedirect.com

Of twenty-one nicotinic acid analogs assayed against tri-o-cresyl phosphate-induced ataxia in hens, five provided partial relief of the syndrome. These were nicotinamide, nikethamide, phenyl nicotinate, 3-picoline, and 3-acetylpyridine. Almost all of those assayed in mice against tri-n-butyl phosphate provided some relief of the paralysis, under the conditions of test, but 1-methylnicotinamide and nicotinamide-1-oxide were inactive. 1-Methyl-2-oxo-1,2-dihydronicotinamide and 1-methyl-6-oxo-1,6-dihydronicotinamide delayed the knockdown due to TBP, as did the ethyl and phenyl esters of 1-methyl-6-oxo-1,2-dihydronicotinic acid. Compounds with other 1-alkyl substituents were not very active or were inactive. The structure-activity requirements for the TBP or tubocurarine assays were almost parallel, indicating that the action of TBP is at the same site as tubocurarine, that is, at the neuromuscular junction. Protective activity was obtained with phenyl 1-methyl-6-oxo-1,6-dihydronicotinate against only those toxicants which block impulse transmission at this junction, but the fact that the decamethonium-induced block was relieved was interpreted to mean that the protective action is probably not due to inhibition of acetylcholinesterase.These results indicate, but do not establish, that the protective activity of nicotinic acid analogs against TBP and tubocurarine is derived from a pyridone metabolite. In any case, the potential usefulness of these pyridone derivatives as anticurare agents warrants further investigation.

We also recommend Trading Suppliers and Manufacturers of (Z)-3-(Dimethoxyphosphinyloxy)-2-butenoic acid (cas 19491-70-4). Pls Click Website Link as below: cas 19491-70-4 suppliers