Lee S H, Kayser V, Guilbaud G
Unité de Recherches de Physiopharmacologie du Système Nerveux, INSERM U 161, Paris, France.
Eur J Pharmacol. 1994 Oct 13;264(1):61-7. doi: 10.1016/0014-2999(94)90636-x.
The antinociceptive effect of i.v. kelatorphan (2.5, 5, 10 and 15 mg/kg), a mixed inhibitor of enkephalin degrading enzymes, was studied in a rat model of peripheral unilateral mononeuropathy (chronic constriction of the common sciatic nerve). Kelatorphan at 2.5 and 5 mg/kg had no significant effect on the vocalization threshold to paw pressure test, but higher doses (10 mg/kg) produced a significant antinociceptive effect which plateaued at 15 mg/kg, on both hindpaws. Kelatorphan (10 mg/kg) was co-injected with the specific mu-, delta- and kappa-opioid receptor antagonists naloxone (0.1 mg/kg), naltrindole (1 mg/kg) or nor-binaltorphimine (1 mg/kg). The effect of kelatorphan 10 mg/kg was completely prevented by naloxone, reduced by 75% by naltrindole (both hindpaws), and reduced by 50% by nor-binaltorphimine (contralateral paw only).
在大鼠外周单侧单神经病（坐骨神经慢性缩窄）模型中，研究了静脉注射脑啡肽降解酶混合抑制剂凯拉托啡（2.5、5、10和15毫克/千克）的抗伤害感受作用。2.5和5毫克/千克的凯拉托啡对 paw 压力测试的发声阈值没有显著影响，但较高剂量（10毫克/千克）产生了显著的抗伤害感受作用，在15毫克/千克时达到平稳，对双侧后爪均有此作用。将凯拉托啡（10毫克/千克）与特异性μ、δ和κ阿片受体拮抗剂纳洛酮（0.1毫克/千克）、纳曲吲哚（1毫克/千克）或去甲二氢吗啡酮（1毫克/千克）共同注射。10毫克/千克的凯拉托啡的作用被纳洛酮完全阻断，被纳曲吲哚（双侧后爪）降低75%，被去甲二氢吗啡酮（仅对侧爪）降低50%。
