Li Wei, Hao Jing-lai, Tang Yun, Chen Yan, Qiu Zhui-bai
Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 200032, China.
Acta Pharmacol Sin. 2005 Mar;26(3):334-8. doi: 10.1111/j.1745-7254.2005.00045.x.
To investigate the mechanism of action of a potent analgesic, (+/-)-meptazinol.
The structures of meptazinol enantiomers were compared with opioid pharmacophore and tramadol.
Neither enantiomer of meptazinol fitted any patterns among the opioid pharmacophore and tramadol, although they did share some structural and pharmacological similarities. However, the structure superpositions implied that both enantiomers of meptazinol might share some similar analgesic mechanisms with typical opiate analgesics.
Meptazinol should have a different mechanism of action to known analgesics, which would be helpful in further investigations of meptazinol in the search for non-addictive analgesics.
研究强效镇痛药(±)-美普他酚的作用机制。
将美普他酚对映体的结构与阿片类药物药效团及曲马多进行比较。
美普他酚的两种对映体均不符合阿片类药物药效团和曲马多的任何模式,尽管它们确实有一些结构和药理学上的相似之处。然而,结构叠加表明美普他酚的两种对映体可能与典型的阿片类镇痛药有一些相似的镇痛机制。
美普他酚的作用机制应与已知镇痛药不同,这将有助于在寻找非成瘾性镇痛药的研究中对美普他酚进行进一步研究。