The analgesic effects of R(+)-WIN 55,212-2 mesylate, a high affinity cannabinoid agonist, in a rat model of neuropathic pain
The analgesic effects of R(+)-WIN 55,212-2 mesylate, a high affinity cannabinoid agonist, in a rat model of neuropathic pain
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DOI：
10.1016/s0304-3940(96)13308-5
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发表时间：
1997-01-17
影响因子：
2.5
通讯作者：
Kopin, IJ
中科院分区：
文献类型：
--
作者：
Herzberg, U;Eliav, E;Kopin, IJ
高亲和力大麻素受体激动剂的效果进行了评估，在大鼠慢性坐骨神经（CCI）或假手术的压迫性损伤。腹膜内（i. p.）注射活性对映体而非活性对映体以剂量依赖性方式减轻了CCI动物表现出的疼痛行为。此外，在0.43 - 4.3 mg/kg剂量范围内，在坐骨神经结扎对侧爪和接受假手术的动物中均未观察到对热刺激敏感性的影响。接受CCI并用4.3 mg/kg处理的动物在结扎的坐骨神经同侧的爪中表现出痛觉减退，即热痛觉减退完全逆转。痛觉减退被认为是暴露感觉缺陷的结果，反映了CCI的C和A δ的已知损失。虽然副作用存在于一些CCI动物经受高剂量（4.3mg/kg），中等剂量（2.14mg/kg）完全缓解热和机械痛觉过敏，和机械异常性疼痛而没有副作用。除了确定用于疼痛性神经病的潜在药物治疗之外，本研究表明大麻素受体的变化发生在神经损伤的动物中。(C)1997 Elsevier Science爱尔兰有限公司
The effects of a high affinity cannabinoid receptor agonist were evaluated in rats subjected to chronic constriction injury of the sciatic nerve (CCI) or a sham operation. Intraperitoneal (i.p.) injections of the active, but not the inactive enantiomer, alleviated the pain behavior exhibited by CCI animals in a dose dependent manner. Moreover, at doses ranging from 0.43 to 4.3 mg/kg effects on sensitivity to a heat stimulus were observed neither in the paw contralateral to the sciatic ligation, nor in animals subjected to sham surgery. Animals subjected to CCI and treated with 4.3 mg/kg exhibited hypoalgesia in the paw ipsilateral to the ligated sciatic, i.e. heat hypoalgesia was completely reversed. The hypoalgesia is presumed to be the results of unmasking of a sensory deficit reflecting the known loss of C and A delta with CCI. Although side effects were present in some CCI animals subjected to the high dose (4.3 mg/kg), a moderate dose (2.14 mg/kg) completely alleviated the thermal and mechanical hyperalgesia, and mechanical allodynia without side effects, In addition to identifying a potential drug treatment for painful neuropathy, this study suggests that changes in cannabinoid receptors occurs in nerve injured animals. (C) 1997 Elsevier Science Ireland Ltd.