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某些取代水杨酸在完整大鼠体内作为代谢刺激剂的相对效力。

The relative potencies of some substituted salicylic acids as metabolic stimulants in the intact rat.

作者信息

ANDREWS M M

出版信息

Br J Pharmacol Chemother. 1958 Dec;13(4):419-23. doi: 10.1111/j.1476-5381.1958.tb00232.x.

Abstract

The effects of eighteen substituted benzoic acids on the rate of oxygen consumption have been studied in rats. 2:3-Dihydroxybenzoic acid, phthalic acid and 6-methylsalicylic acid were, at the doses used, inactive; m- and p-hydroxybenzoic acid, 2:4-, 2:5-, 2:6-, 3:4-, and 3:5-dihydroxybenzoic acid, o-aminobenzoic acid, salicyluric acid, salicylamide and 5-aminosalicylic acid decreased the rate of oxygen consumption. Only salicylic acid and o-, m- and p-cresotic acid (3-, 4- and 5-methylsalicylic acid respectively) increased the rate of oxygen consumption. Molar potency ratios of the cresotic acids as metabolic stimulants relative to salicylic acid were determined; o-cresotic acid was the most powerful with a ratio of 2.61, m- and pcresotic acid had values of 1.78 and 1.89 respectively. Two possible explanations of the higher potencies of the cresotic acids were considered. No difference in the primary action of the drug was established by determining the effect on rate of oxygen consumption of a mixture of o-cresotic and salicylic acids. An alternative possibility was that the rates of detoxication and excretion of the cresotic acids differed among themselves and from salicylic acid. No such differences were found.

摘要

研究了18种取代苯甲酸对大鼠耗氧率的影响。在所使用的剂量下,2,3 - 二羟基苯甲酸、邻苯二甲酸和6 - 甲基水杨酸无活性;间羟基苯甲酸、对羟基苯甲酸、2,4 -、2,5 -、2,6 -、3,4 -和3,5 - 二羟基苯甲酸、邻氨基苯甲酸、水杨尿酸、水杨酰胺和5 - 氨基水杨酸降低了耗氧率。只有水杨酸和邻、间、对甲酚酸(分别为3 -、4 -和5 - 甲基水杨酸)提高了耗氧率。测定了甲酚酸作为代谢刺激剂相对于水杨酸的摩尔效价比;邻甲酚酸最有效,比值为2.61;间甲酚酸和对甲酚酸的值分别为1.78和1.89。考虑了甲酚酸效力较高的两种可能解释。通过测定邻甲酚酸和水杨酸混合物对耗氧率的影响,未发现药物的主要作用有差异。另一种可能性是甲酚酸的解毒和排泄速率彼此不同,且与水杨酸不同。但未发现此类差异。

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