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美索巴莫对映体在小鼠体内的肌肉松弛活性。

Muscle relaxant activity of methocarbamol enantiomers in mice.

作者信息

Souri E, Sharifzadeh M, Farsam H, Gharavi N

机构信息

Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Iran.

出版信息

J Pharm Pharmacol. 1999 Jul;51(7):853-5. doi: 10.1211/0022357991773069.

Abstract

Documented studies support the emerging idea that drug enantiomers could have different pharmacological activity. Our bibliographical data have shown that so far no report has been published on the pharmacological activity of individual enantiomers of methocarbamol. This study was conducted to characterize the muscle relaxant activity of methocarbamol enantiomers. The rotarod test was used to compare the muscle relaxant activity of racemic methocarbamol and pure enantiomers after intraperitoneal administration of the enantiomers to mice. The results show that (+)-R-methocarbamol has higher muscle relaxant activity compared with racemic methocarbamol or (-)-S-methocarbamol.

摘要

有文献记载的研究支持了药物对映体可能具有不同药理活性这一新兴观点。我们的文献数据表明,到目前为止,尚未有关于美索巴莫单个对映体药理活性的报道。本研究旨在表征美索巴莫对映体的肌肉松弛活性。采用转棒试验比较了消旋美索巴莫和纯对映体对小鼠腹腔注射后肌肉松弛活性。结果表明,与消旋美索巴莫或(-)-S-美索巴莫相比,(+)-R-美索巴莫具有更高的肌肉松弛活性。

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