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依他佐辛(l-1,4-二甲基-10-羟基-2,3,4,5,6,7-六氢-1,6-亚甲基-1H-4-苯并氮杂䓬)的药理作用。(V)。依他佐辛、喷他佐辛和吗啡连续给药后耐受性形成能力的比较

[Pharmacological action of eptazocine (l-1,4-dimethyl-10-hydroxy-2,3,4,5,6,7-hexahydro-1,6-methano-1H-4-benz azonine). (V). A comparison of eptazocine, pentazocine and morphine with regard to ability of tolerance development after successive administration].

作者信息

Nabeshima T, Yamada S, Kameyama T

出版信息

Nihon Yakurigaku Zasshi. 1986 Jun;87(6):619-27. doi: 10.1254/fpj.87.619.

Abstract

It was investigated whether tolerance to the pharmacological actions and cross-tolerance between eptazocine and pentazocine/morphine were developed by successive administration of eptazocine. In the experiments of mice, successive administration of eptazocine failed to decrease the pharmacological actions of eptazocine on the acetic acid-induced writhing, the pressure and the wheel cage methods. Cross-tolerance between eptazocine and pentazocine/morphine was not observed. Tolerance to the actions of pentazocine and morphine was developed on the wheel cage and the acetic acid-induced writhing/pressure methods, respectively. Cross-tolerance between pentazocine and morphine was also developed on the pressure method. On the tail flick method of rats, tolerance to the action of eptazocine was observed, similar to morphine, but not cross-tolerance between eptazocine and morphine. These results suggest that there is species difference between mice and rats with regard to the ability of tolerance development and that the mechanisms of tolerance development between eptazocine and pentazocine/morphine may be different since eptazocine failed to show cross tolerance to these analgesics.

摘要

通过连续给予依他佐辛,研究了对其药理作用的耐受性以及依他佐辛与喷他佐辛/吗啡之间的交叉耐受性是否会产生。在小鼠实验中,连续给予依他佐辛未能降低依他佐辛对醋酸诱导扭体、压力和转笼法的药理作用。未观察到依他佐辛与喷他佐辛/吗啡之间的交叉耐受性。分别在转笼法和醋酸诱导扭体/压力法上对喷他佐辛和吗啡的作用产生了耐受性。在压力法上也产生了喷他佐辛和吗啡之间的交叉耐受性。在大鼠的甩尾法实验中,观察到对依他佐辛的作用产生了耐受性,类似于吗啡,但依他佐辛与吗啡之间未产生交叉耐受性。这些结果表明,在耐受性产生能力方面,小鼠和大鼠之间存在种属差异,并且依他佐辛与喷他佐辛/吗啡之间耐受性产生的机制可能不同,因为依他佐辛对这些镇痛药未表现出交叉耐受性。

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