ON THE EFFECTS OF SKF 525-A, CARONAMIDE, PROBENECID, SALICYLATE AND ASPIRIN ON THE BIOACETYLATION OF SULFANILAMIDE AND CHOLINE

[摘要] References(19)Cited-By(5)β-Diethylaminoethyldiphenylpropylacetate (SKF 525-A), the typical potent potentiator newly discovered, enhances without having any action for itself, the pharmacological actions of hypnotics, analgesics, central excitants and others (1, 2). As for its mechanism of action, depression of the side chain oxidation, hydroxilation, splitting of ether linkage, dealkylation and deamination in the organism have been reported (3-6). However, there is as yet no report on its effect on acetylation, another important reaction of detoxication.Caronamide, the penicillin potentiator, and benemid (probenecid), the potentiator of penicillin, p-aminosalicylate and diodrast and the accelerator of the uric acid excretion, compete with these remedies for coenzyme-A, thus depressing the enzyme system of the renal tubules in charge of excreting organic substances and consequently delaying excretion of the remedies (7). Salicylate and aspirin act similarly, and prolong the duration of action of penicillin and barbital (8).The essential component of acetylation is also the coenzyme-A. With energy supplied by adenosine triphosphate and the catalysis of transacetylases, coenzyme-A first combines with acetate or citrate to produce acetylcoenzyme-A, which then performs acetylation of sulfonamide, choline and other substances with the help of acetokinases (9-11).We thought, therefore, it worthwhile to study the effects of these potentiators on the bioacetylation of choline and sulfanilamide. At the same time, their effects on cholinesterase which splits and detoxifies acetylcholine have been investigated.

[学科分类] 药理学