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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.

DOI:10.1212/wnl.35.9.1311
PMID:4022377
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。

相似文献

1
Opiate antagonist WIN44,441-3 stereospecifically improves neurologic recovery after ischemic spinal injury.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。
Neurology. 1985 Sep;35(9):1311-5. doi: 10.1212/wnl.35.9.1311.
2
Motor dysfunction after spinal cord injury is mediated by opiate receptors.脊髓损伤后的运动功能障碍是由阿片受体介导的。
Peptides. 1985;6 Suppl 1:15-7. doi: 10.1016/0196-9781(85)90006-3.
3
Naloxone in experimental spinal cord ischemia: dose-response studies.纳洛酮用于实验性脊髓缺血:剂量反应研究。
Eur J Pharmacol. 1984 Aug 3;103(1-2):115-20. doi: 10.1016/0014-2999(84)90196-1.
4
Role of thyrotropin-releasing hormone and opiate receptor antagonists in limiting central nervous system injury.促甲状腺激素释放激素和阿片受体拮抗剂在限制中枢神经系统损伤中的作用。
Adv Neurol. 1988;47:531-46.
5
New pharmacologic approaches to spinal cord injury: opiate antagonists and thyrotropin-releasing hormone.
Cent Nerv Syst Trauma. 1985 Spring;2(1):5-8. doi: 10.1089/cns.1985.2.5.
6
Comparison of the neuroprotective effects of the N-methyl-D-aspartate antagonist MK-801 and the opiate-receptor antagonist nalmefene in experimental spinal cord ischemia.
Arch Neurol. 1990 Mar;47(3):277-81. doi: 10.1001/archneur.1990.00530030043014.
7
Opiate-receptor antagonist nalmefene improves neurological recovery after traumatic spinal cord injury in rats through a central mechanism.阿片受体拮抗剂纳美芬通过中枢机制改善大鼠创伤性脊髓损伤后的神经功能恢复。
J Pharmacol Exp Ther. 1988 May;245(2):742-8.
8
Treatment of experimental stroke with the opiate antagonist win 44,441-3 effects on neurologic function, infarct size, and survival.用阿片拮抗剂WIN 44,441-3治疗实验性中风对神经功能、梗死面积和存活率的影响。
NIDA Res Monogr. 1986;75:531-4.
9
Opiate antagonist improves neurologic recovery after spinal injury.
Science. 1981 Jan 30;211(4481):493-4. doi: 10.1126/science.7455690.
10
Evaluation of the calcium channel antagonist nimodipine in experimental spinal cord ischemia.钙通道拮抗剂尼莫地平在实验性脊髓缺血中的评估。
J Neurosurg. 1984 Apr;60(4):796-9. doi: 10.3171/jns.1984.60.4.0796.

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PLoS One. 2012;7(5):e37798. doi: 10.1371/journal.pone.0037798. Epub 2012 May 25.
2
Prostaglandin derivative PGBx improves neurologic recovery after ischemic spinal injury.前列腺素衍生物PGBx可改善缺血性脊髓损伤后的神经功能恢复。
Pharm Res. 1987 Apr;4(2):130-2. doi: 10.1023/a:1016466902877.