CAM与κ阿片受体激动剂的阿片样物质活性比较。

Comparison of the opioid activity of CAM and kappa agonists.

作者信息

Furst S, Friedmann T, Kovacs A, Wagner T

机构信息

Department of Pharmacology, Semmelweis University of Medicine, Budapest, Hungary.

出版信息

NIDA Res Monogr. 1986;75:224-7.

PMID:2828975

Abstract

CAM has been shown to produce opiate agonist and antagonist activities. Based on its potent agonist activity in rabbit vas deferens and the low potency of naloxone to antagonize its agonist effect in the guinea pig ileum and mouse vas deferens, CAM can be considered as kappa agonist. It is further supported by its diuretic effect and the estimated "apparent pA2" values with naloxone and Mr-2266BS. However, in the rabbit ear artery and cat nictitating membrane, ethylketazocine (EK) produced agonist activity, while CAM produced antagonist activity. Also, EK differs from CAM in mouse vas deferens in the presence of 4-aminopyridine. It is concluded, that CAM might be an agonist on kappa type (subtype) of opiate receptors, although its spectrum of activity was found to be different from EK or bremazocine.

摘要

已证明骆驼蓬碱具有阿片激动剂和拮抗剂活性。基于其在兔输精管中的强效激动剂活性以及纳洛酮在豚鼠回肠和小鼠输精管中拮抗其激动剂作用的低效性，骆驼蓬碱可被视为κ激动剂。其利尿作用以及与纳洛酮和Mr - 2266BS的估计“表观pA2”值进一步支持了这一点。然而，在兔耳动脉和猫瞬膜中，乙基酮佐辛（EK）产生激动剂活性，而骆驼蓬碱产生拮抗剂活性。此外，在存在4 - 氨基吡啶的情况下，EK在小鼠输精管中的作用与骆驼蓬碱不同。得出的结论是，骆驼蓬碱可能是阿片受体κ型（亚型）的激动剂，尽管发现其活性谱与EK或布马佐辛不同。