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贝司他汀,一种氨肽酶B抑制剂,可选择性降低大鼠的酒精摄入量。

Bestatin, an aminopeptidase B inhibitor, selectively reduces alcohol intake in rats.

作者信息

Szczepanska R, Grupp L A

机构信息

Primary Mechanisms Department, Addiction Research Foundation of Ontario, Toronto, Canada.

出版信息

Alcohol Clin Exp Res. 1993 Apr;17(2):434-7. doi: 10.1111/j.1530-0277.1993.tb00790.x.

Abstract

Extensive research has shown that manipulations that augment activity in the renin-angiotensin system can reduce alcohol intake. Inhibition of aminopeptidase B and M can prolong the action of angiotensin (ANG) II and ANG III by preventing their degradation. This study assessed the ability of bestatin, an aminopeptidase B and M inhibitor, to decrease alcohol intake. Bestatin produced a dose-dependent reduction in alcohol intake without altering water intake. The angiotensin antagonist Sar1Thr3-ANG II, however, did not attenuate the effect of bestatin, suggesting that the reduction in alcohol intake was mediated by a system other than the renin-angiotensin system. Bestatin (Ubenimex) is used extensively in Japan as an anticancer agent. It has a low toxicity and is readily absorbed after oral administration. Although further research is needed to uncover the mechanism of its effect, the potential of this drug as an adjunct for the treatment of alcohol abuse should be evaluated.

摘要

大量研究表明,增强肾素-血管紧张素系统活性的操作可减少酒精摄入量。抑制氨肽酶B和M可通过阻止血管紧张素(ANG)II和ANG III的降解来延长它们的作用时间。本研究评估了氨肽酶B和M抑制剂贝司他汀减少酒精摄入量的能力。贝司他汀可使酒精摄入量呈剂量依赖性减少,而不改变水的摄入量。然而,血管紧张素拮抗剂Sar1Thr3-ANG II并未减弱贝司他汀的作用,这表明酒精摄入量的减少是由肾素-血管紧张素系统以外的其他系统介导的。贝司他汀(乌苯美司)在日本被广泛用作抗癌药物。它毒性低,口服后易于吸收。尽管需要进一步研究以揭示其作用机制,但该药物作为酒精滥用治疗辅助药物的潜力应予以评估。

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