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一种新型阿片样肽,[D-精氨酸2,β-丙氨酸4]-皮啡肽四肽;小鼠的身体依赖性倾向

A new class opioid peptide, [D-Arg2, beta-Ala4]-dermorphin tetrapeptide; physical dependence liability in mice.

作者信息

Chaki K, Sakurada S, Sakurada T, Sato T, Kawamura S, Kisara K, Sasaki Y, Suzuki K

机构信息

Department of Pharmacology, Tohoku College of Pharmacy, Sendai, Japan.

出版信息

Neuropeptides. 1989 Feb-Mar;13(2):83-8. doi: 10.1016/0143-4179(89)90003-6.

Abstract

Development of morphine-like physical dependence of the [D-Arg2, beta-Ala4]-dermorphin tetrapeptide (H-Tyr-D-Arg-Phe-beta-Ala-OH) has been evaluated and compared with the physical dependence liability of morphine or pentazocine. Degree of the physical dependence was assessed by the naloxone-precipitated jumping behaviour in mice after treatment of a single dose of each compound. The number of jumps and the time of latency to first jump were recorded in this experiment. Number of jumps in a group pretreated with the peptide showed less than that in morphine-treated group. In addition, latency to the appearance of the first jump in the peptide-treated mice was later than that in the morphine-treated group. The present results indicate that the physical dependence induced by [D-Arg2, beta-Ala4]-dermorphin tetrapeptide may be less marked than that produced by morphine. It is also interesting to note that the antinociceptive effect of this opioid peptide is more powerful and of longer duration than that induced by morphine or pentazocine.

摘要

已对[D-精氨酸2,β-丙氨酸4]-皮啡肽四肽(H-酪氨酸-D-精氨酸-苯丙氨酸-β-丙氨酸-OH)类吗啡身体依赖性的发展进行了评估,并与吗啡或喷他佐辛的身体依赖性倾向进行了比较。通过在小鼠单次给予每种化合物后用纳洛酮诱发的跳跃行为来评估身体依赖性的程度。在该实验中记录跳跃次数和首次跳跃的延迟时间。用该肽预处理的组中的跳跃次数少于吗啡处理组。此外,肽处理小鼠中首次跳跃出现的延迟时间比吗啡处理组更晚。目前的结果表明,[D-精氨酸2,β-丙氨酸4]-皮啡肽四肽诱导的身体依赖性可能不如吗啡产生的明显。同样有趣的是,这种阿片肽的镇痛作用比吗啡或喷他佐辛诱导的更强且持续时间更长。

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