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γ-丁酸甜菜碱的结构类似物米屈肼([3-(2,2,2-三甲基肼基)丙酸酯])对依赖肉碱的动态代谢的影响

[The effect of a structural analog of gamma-butyrobetaine, mildronate, [3-2,2,2-trimethylhydrazine)propionate] on dynamic carnitine-dependent metabolism].

作者信息

Shutenko Zh V, Priedena I A, Kalvin'sh I Ia, Lukevits E Ia

出版信息

Vopr Med Khim. 1991 May-Jun;37(3):24-6.

PMID:1949676
Abstract

Inhibitor of carnitine-dependent metabolism mildronate, 3-(2,2,2-trimethylhydrazinium) propionate, administered into rats at a dose of 200 mg/kg, per os, within 10 days, caused a decrease in concentration of free carnitine and of long-chain acylcarnitine in myocardium as well as contributed to accumulation of free fatty acids in blood serum. Besides, the rate of I-14C-palmitic acid turnover to 14CO2 was decreased in myocardium homogenate. The drug inhibitory effect on carnitine biosynthesis from gamma-butyrobetaine was responsible for the phenomenon observed. Content of the metabolites studied was altered gradually both during treatment of rats with mildronate and after the drug abolition, thus demonstrating an opportunity of gentle influence on carnitine-dependent metabolism by means of the drug treatment and its abolition.

摘要

肉碱依赖性代谢抑制剂米屈肼(3-(2,2,2-三甲基肼基)丙酸酯)以200mg/kg的剂量经口给予大鼠,持续10天,导致心肌中游离肉碱和长链酰基肉碱浓度降低,并促使血清中游离脂肪酸积累。此外,心肌匀浆中I-14C-棕榈酸向14CO2的周转速率降低。该药物对γ-丁酸甜菜碱合成肉碱的抑制作用导致了所观察到的现象。在用米屈肼治疗大鼠期间以及停药后,所研究代谢物的含量均逐渐改变,从而表明通过药物治疗及其停用对肉碱依赖性代谢进行温和影响的可能性。

相似文献

1
[The effect of a structural analog of gamma-butyrobetaine, mildronate, [3-2,2,2-trimethylhydrazine)propionate] on dynamic carnitine-dependent metabolism].γ-丁酸甜菜碱的结构类似物米屈肼([3-(2,2,2-三甲基肼基)丙酸酯])对依赖肉碱的动态代谢的影响
Vopr Med Khim. 1991 May-Jun;37(3):24-6.
2
[Effect of a new structural analog of gamma-butyrobetaine-- 3-(2,2,2-trimethylhydrazine)propionate (THP) on carnitine level, carnitine-dependent fatty acid oxidation and various indices of energy metabolism in the myocardium].
Vopr Med Khim. 1986 Jul-Aug;32(4):72-6.
3
[The effect of mildronate on disorders of the cardiac contractile function in rats caused by an excess of free fatty acids and ischemia].
Farmakol Toksikol. 1990 Sep-Oct;53(5):27-9.
4
[Potentiation of the antiketogenic effect of exogenous glucose with the help of the new beta-oxidation inhibitor mildronate--3-(2,2,2-trimethylhydrazine)propionate].
Vopr Med Khim. 1991 Mar-Apr;37(2):59-60.
5
[Effect of DL-carnitine and gamma-butyrobetaine hydroxylase inhibitor 3-(2,2,2-trimethylhydrazinium) propionate on isoproterenol-induced changes in the metabolism of the rat myocardium].[DL-肉碱和γ-丁甜菜碱羟化酶抑制剂3-(2,2,2-三甲基肼基)丙酸对异丙肾上腺素诱导的大鼠心肌代谢变化的影响]
Vopr Med Khim. 1988 Sep-Oct;34(5):30-4.
6
[The effect of mildronate on carnitine-dependent and carnitine-independent ketogenesis in rats].
Farmakol Toksikol. 1991 Jul-Aug;54(4):41-2.
7
[Study of the effect of an inhibitor of carnitine-dependent metabolism of mildronate on the oxidation of fatty acids in the liver mitochondria of intact rats].[米屈肼对肉碱依赖性代谢的抑制剂对完整大鼠肝脏线粒体中脂肪酸氧化作用的研究]
Vopr Med Khim. 1991 Mar-Apr;37(2):44-6.
8
[Regulation of carnitine-dependent metabolism of fatty acids in the rat myocardium using 3-(2,2,2-trimethylhydrazinium) propionate].
Vopr Med Khim. 1989 Mar-Apr;35(2):59-64.
9
[Biochemical characteristics of the anti-ischemic action of the new structural analog of gamma-butyrobetaine 3-(2,2,2,-trimethylhydrazine)propionate].
Farmakol Toksikol. 1987 Mar-Apr;50(2):100-4.
10
Mildronate, an inhibitor of carnitine biosynthesis, induces an increase in gamma-butyrobetaine contents and cardioprotection in isolated rat heart infarction.米屈肼,一种肉碱生物合成抑制剂,可使γ-丁酸甜菜碱含量增加,并对离体大鼠心脏梗死产生心脏保护作用。
J Cardiovasc Pharmacol. 2006 Dec;48(6):314-9. doi: 10.1097/01.fjc.0000250077.07702.23.