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美普他酚对豚鼠离体回肠的作用能通过抑制乙酰胆碱酯酶来解释吗?

Can the effects of meptazinol on the guinea-pig isolated ileum be explained by inhibition of acetylcholinesterase?

作者信息

Ennis C, Haroun F, Lattimer N

出版信息

J Pharm Pharmacol. 1986 Jan;38(1):24-7. doi: 10.1111/j.2042-7158.1986.tb04461.x.

Abstract

It has previously been shown that there is a cholinergic component in the antinociceptive action of the opioid analgesic drug meptazinol. In the present study meptazinol was shown to be an inhibitor of acetylcholinesterase in-vitro with a potency one hundredth that of physostigmine. This activity was found to reside only in the (-)-enantiomer of meptazinol. The anticholinesterase activity of meptazinol may explain the increase in the size of the electrically-evoked contraction of the guinea-pig isolated ileum preparation since by using a long pulse width (5 ms) it was found that the (-)-enantiomer of meptazinol modified only the component of the response due to neuronally released acetylcholine and had no direct effect on the smooth muscle. This property of meptazinol may also be responsible for the cholinergic effects of the drug in-vivo.

摘要

先前的研究表明,阿片类镇痛药美普他酚的抗伤害感受作用中存在胆碱能成分。在本研究中,美普他酚在体外被证明是乙酰胆碱酯酶的抑制剂,其效力为毒扁豆碱的百分之一。发现这种活性仅存在于美普他酚的(-)-对映体中。美普他酚的抗胆碱酯酶活性可能解释了豚鼠离体回肠标本电诱发收缩幅度的增加,因为通过使用长脉冲宽度(5毫秒)发现,美普他酚的(-)-对映体仅改变了神经元释放的乙酰胆碱引起的反应成分,对平滑肌没有直接影响。美普他酚的这一特性也可能是该药物体内胆碱能效应的原因。

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