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阿片拮抗剂WIN44,441-3可立体特异性地改善缺血性脊髓损伤后的神经功能恢复。

Opiate antagonist WIN44,441-3 stereospecifically improves neurologic recovery after ischemic spinal injury.

作者信息

Faden A I, Jacobs T P

出版信息

Neurology. 1985 Sep;35(9):1311-5. doi: 10.1212/wnl.35.9.1311.

Abstract

In the unanesthetized rabbit, temporary aortic occlusion results in predictable patterns of spinal cord injury. We use this "spinal stroke" model to assess the potential role of opiate antagonists in treating CNS ischemia. WIN44,441-3 (WIN(-], an opiate antagonist with enhanced activity at the kappa-receptor, reduced motor dysfunction after ischemic spinal cord injury. The effect was stereospecific and dose-related; beneficial actions were seen at doses as low as 40 micrograms/kg. Opiate receptor antagonists may be therapeutically useful in ischemic CNS injury, and the beneficial actions of these compounds may be at the kappa-receptor site.

摘要

在未麻醉的兔子中,暂时性主动脉闭塞会导致可预测的脊髓损伤模式。我们使用这种“脊髓中风”模型来评估阿片类拮抗剂在治疗中枢神经系统缺血方面的潜在作用。WIN44,441-3(WIN(-])是一种对κ受体具有增强活性的阿片类拮抗剂,可减轻缺血性脊髓损伤后的运动功能障碍。这种作用具有立体特异性且与剂量相关;在低至40微克/千克的剂量下即可观察到有益作用。阿片受体拮抗剂可能对缺血性中枢神经系统损伤具有治疗作用,并且这些化合物的有益作用可能发生在κ受体部位。

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