芬太尼——一种有效的阿片类镇痛药:综述

A. Sharma, Maniratna Nareda, Sanaa Aziz, Deepak Sharma, S. Garg
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引用次数: 7

摘要

芬太尼是一种强效镇痛药,药效几乎是吗啡的100倍,芬太尼作为止痛剂和麻醉剂的使用在医学上被广泛采用。芬太尼于1959年由詹森博士首次引入。许多类型的芬太尼衍生物都是通过在正分子上加入相应的取代基来改变其效价而被开发出来的,一些相关分子可能以异构体的形式存在。(3-甲基芬太尼的异构体),根据使用的不同,它们具有不同类型的镇痛效力。Bever报道了一个甲基(-CH3)进入哌啶环的第3位,增加了镇痛效力。反式异构体的活性略高于芬太尼,但其各自的顺式形式的活性高8倍。他们发现顺式(+)3-甲基芬太尼的活性比芬太尼更强,而顺式阴性形式的活性则更弱。
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Fentanyl - A Potent Opioid Analgesic: A Review
Fentanyl is a potent analgesic that is almost a hundred times accented than morphine, the use of fentanyl is pain allayer and anesthetic was adopted in the medical primed. Fentanyl was first introduced by Dr. Jansen in 1959. Many type of fentanyl derivatives have been developed by adding respective substituents to the canonic molecule inorder to alter the potency, some of the ensunting molecules may exist as isomers. (The isomers of 3-methylfentanyl), which have different types of analgesic potencies depends on which is used. Bever reported that the 3rd position of a methyl group (-CH3) into the piperidine ring, increases analgesic potency. The Trans isomer was slightly more active agent than fentanyl, but its respective cis form was eight folds more active. They found that activity of the cis (+) 3-methylfentanyl more potent than fentanyl, whereas the cis negative form was less potent.
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