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[依托唑啉(l-1,4-二甲基-10-羟基-2,3,4,5,6,7-六氢-1,6-亚甲基-1H-4-苯并吖庚因)的药理作用。依托唑啉对自发运动的影响]

[Pharmacological action of eptazocine (l-1,4-dimethyl-10-hydroxy-2,3,4,5,6,7-hexahydro-1,6-methano-1H-4-benzazonine). Effects of eptazocine on spontaneous movements].

作者信息

Sakakibara S

出版信息

Nihon Yakurigaku Zasshi. 1983 Jun;81(6):549-63.

PMID:6618345
Abstract

The effects of eptazocine on spontaneous movements in mice were investigated by using a multi-dimensional behavioral analyzer (Animex II) in comparison with those of pentazocine and morphine. Eptazocine at 20, 40 and 80 mg/kg increased the spontaneous movements in a dose-dependent fashion. On the contrary, the spontaneous movements in mice were significantly decreased by pentazocine in the same dose range. On the other hand, morphine produced biphasic effects: 20 mg/kg morphine inhibited the spontaneous movements, but it potentiated them at doses of 40 and 80 mg/kg. The effects of these three drugs on the spontaneous movements were antagonized by naloxone. The effects of pentazocine and morphine on the spontaneous movements were modified by the successive administration of these drugs, but not by eptazocine administration. The eptazocine-induced hyperactive movements were potentiated by apomorphine and were inhibited by haloperidol, alpha-methyl-p-tyrosine and disulfiram. On the contrary, the inhibitory effects of pentazocine on the spontaneous movements were antagonized by apomorphine. On the other hand, the inhibitory effects of 20 mg/kg morphine on the spontaneous movements were also inhibited by apomorphine and haloperidol. These results suggest that the pharmacological effects of eptazocine on the spontaneous movements in mice are different from those of pentazocine and morphine. The effects of eptazocine may be mediated by opiate receptors and catecholaminergic neurons, but the potency of eptazocine to induce tolerance is less than pentazocine and morphine.

摘要

使用多维度行为分析仪(Animex II)研究了依托唑啉对小鼠自发活动的影响,并与喷他佐辛和吗啡进行了比较。20、40和80mg/kg的依托唑啉以剂量依赖性方式增加自发活动。相反,在相同剂量范围内,喷他佐辛显著降低了小鼠的自发活动。另一方面,吗啡产生双相作用:20mg/kg吗啡抑制自发活动,但在40和80mg/kg剂量时增强自发活动。这三种药物对自发活动的影响均被纳洛酮拮抗。喷他佐辛和吗啡对自发活动的影响会因连续给药而改变,但依托唑啉给药不会产生这种影响。阿扑吗啡增强了依托唑啉诱导的多动,而氟哌啶醇、α-甲基-p-酪氨酸和双硫仑抑制了这种多动。相反,阿扑吗啡拮抗了喷他佐辛对自发活动的抑制作用。另一方面,20mg/kg吗啡对自发活动的抑制作用也被阿扑吗啡和氟哌啶醇抑制。这些结果表明,依托唑啉对小鼠自发活动的药理作用与喷他佐辛和吗啡不同。依托唑啉的作用可能由阿片受体和儿茶酚胺能神经元介导,但依托唑啉诱导耐受性的效力低于喷他佐辛和吗啡。

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[Pharmacological action of eptazocine (l-1,4-dimethyl-10-hydroxy-2,3,4,5,6,7-hexahydro-1,6-methano-1H-4-benzazonine). Effects of eptazocine on spontaneous movements].[依托唑啉(l-1,4-二甲基-10-羟基-2,3,4,5,6,7-六氢-1,6-亚甲基-1H-4-苯并吖庚因)的药理作用。依托唑啉对自发运动的影响]
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