Effect of 2-ethyl-6-methylpyridinol-3-yl-thiooctanoate and its Non-Esterified Components on the Behavior of Rats in an Elevated Plus Maze

IF 0.8 4区 医学 Q4 CHEMISTRY, MEDICINAL
I. A. Volchegorskii, S. I. Grobovoi, A. I. Sinitskii, I. Y. Miroshnichenko, L. M. Rassokhina, R. R. Mihajlov
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Abstract

The effect of thioctic acid (TA), 2-ethyl-6-methyl-3-hydroxypyridine hydrochloride (emoxypine), and their ester derivative (2-ethyl-6-methylpyridinol-3-yl-thiooctanoate, thioxypine) on the behavior of rats in an elevated plus maze (EPM) was studied. Intraperitoneal administration (three times) of TA, emoxypine, and their equimolar mixture in single doses of 36.25, 72.5, and 145 μmol/kg enhanced individual manifestations of anxious behavior in the EPM but did not cause full-blown anxiogenic effects. Similar pro-anxiogenic effects were observed when TA was administered in a dose of 36.25 μmol/kg and emoxypine in doses of 72.5 and 145 μmol/kg. The equimolar mixture of the non-esterified components of thioxypine had a pro-anxiogenic effect in doses of 36.25 and 72.5 μmol/kg. Combination of TA and 2-ethyl-6-methyl-3-hydroxypyridine into the ester potentiated their pro-anxiogenic activity, which manifested as an extensive anxiogenic effect of thioxypine when administered three times in a dose of 145 μmol/kg.

2-乙基-6-甲基吡啶醇-3-基硫代辛酸酯及其非酯化成分对大鼠在高架正迷宫中行为的影响
研究了硫辛酸(TA)、2-乙基-6-甲基-3-羟基吡啶盐酸盐(emoxypine)及其酯衍生物(2-乙基-6-甲基吡啶醇-3-基硫辛酸酯,thioxypine)对大鼠在高架加迷宫(EPM)中行为的影响。以 36.25、72.5 和 145 μmol/kg 的单次剂量腹腔注射(三次)TA、emoxypine 和它们的等摩尔混合物可增强 EPM 中焦虑行为的个别表现,但不会引起全面的致焦虑效应。当 TA 的剂量为 36.25 μmol/kg 和 emoxypine 的剂量为 72.5 和 145 μmol/kg 时,也观察到了类似的促焦虑效应。在剂量为 36.25 和 72.5 μmol/kg 时,硫氧嘧啶非酯化成分的等摩尔混合物具有促兴奋作用。将 TA 和 2-乙基-6-甲基-3-羟基吡啶合并成酯可增强其促焦虑活性,当以 145 μmol/kg 的剂量给药三次时,表现为硫氧嘧啶的广泛促焦虑效应。
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来源期刊
Pharmaceutical Chemistry Journal
Pharmaceutical Chemistry Journal CHEMISTRY, MEDICINAL-PHARMACOLOGY & PHARMACY
CiteScore
1.30
自引率
22.20%
发文量
226
审稿时长
3-8 weeks
期刊介绍: Pharmaceutical Chemistry Journal is a monthly publication devoted to scientific and technical research on the creation of new drugs and the improvement of manufacturing technology of drugs and intermediates. International contributors cover the entire spectrum of new drug research, including: methods of synthesis; results of pharmacological, toxicological, and biochemical studies; investigation of structure - activity relationships in prediction of new compounds; methods and technical facilities used; and problems associated with the development of ecologically safe and economically feasible methods of industrial production. In addition, analytical reviews of the international literature in the field provide coverage of the most recent developments around the world. Pharmaceutical Chemistry Journal is a translation of the Russian journal Khimiko-Farmatsevticheskii Zhurnal. The Russian Volume Year is published in English from April. All articles are peer-reviewed.
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