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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.

DOI:10.1111/j.1476-5381.1958.tb00232.x
PMID:13618547
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1481881/
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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引用本文的文献

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2
THE EFFECTS OF NONCALORIGENIC CONGENERS OF SALICYLATE ON THE PERIPHERAL METABOLISM OF THYROXINE.水杨酸非产热同系物对甲状腺素外周代谢的影响
J Clin Invest. 1964 May;43(5):931-42. doi: 10.1172/JCI104979.
3
The glycogenolytic activity of some substituted salicylic acids.某些取代水杨酸的糖原分解活性。
Biochem J. 1960 May;75(2):298-303. doi: 10.1042/bj0750298.

本文引用的文献

1
The Antirheumatic Effect of Sodium Gentisate.龙胆酸钠的抗风湿作用。
Science. 1948 Sep 10;108(2802):281. doi: 10.1126/science.108.2802.281.
2
Sodium gamma-resorcylate in rheumatic fever.γ-间苯二酚钠在风湿热中的应用
Br Med J. 1951 Aug 11;2(4727):321-6. doi: 10.1136/bmj.2.4727.321.
3
A new outlook on the action of salicylate.水杨酸盐作用的新观点。
Scott Med J. 1957 Mar;2(3):91-6. doi: 10.1177/003693305700200303.
4
Comparison of the metabolic stimulating action of aspirin and thyroid.阿司匹林与甲状腺的代谢刺激作用比较。
Nature. 1956 Aug 4;178(4527):259-60. doi: 10.1038/178259a0.
5
The anti-thyroid action of para-aminosalicylic acid.对氨基水杨酸的抗甲状腺作用。
Lancet. 1954 Nov 6;267(6845):931-6. doi: 10.1016/s0140-6736(54)92552-0.
6
Rapid determination of salicylate in biological fluids.生物流体中水杨酸盐的快速测定。
Biochem J. 1954 Jun;57(2):301-3. doi: 10.1042/bj0570301.
7
Effect of certain hydroxybenzoic acids on the oxygen consumption of Wistar rats.某些羟基苯甲酸对Wistar大鼠耗氧量的影响。
Ann Rheum Dis. 1954 Mar;13(1):60-2. doi: 10.1136/ard.13.1.60.
8
The respiratory effects of salicylate.水杨酸盐对呼吸系统的影响。
Br Med J. 1952 Nov 1;2(4791):964-7. doi: 10.1136/bmj.2.4791.964.