Reche I, Fuentes J A, Ruiz-Gayo M
Departamento de Farmacologia, Facultad de Farmacia, Universidad Complutense de Madrid, Spain.
Eur J Pharmacol. 1996 Apr 22;301(1-3):75-81. doi: 10.1016/0014-2999(96)00045-3.
delta 9-tetrahydrocannabinol elicits analgesia in rodents by both spinal and supraspinal mechanisms. Pharmacological data point to a link between cannabinoids and the opioid system. The lack of specific cannabinoid receptor antagonists has hindered the investigation of the physiological relevance of the cannabinoid system in nociception control. In this work we characterized the effect of the new cannabinoid receptor antagonist, SR-141,716 A (N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-3- pyrazolecarboxamide hydrochloride), on delta 9-tetrahydrocannabinol-induced analgesia. pA2 values in the tail-flick and in lick and jump responses in the hot-plate tests were 9.59, 8.72 and 10.21, respectively. Slope values of pA2 plots were not different from -1 indicating competitive antagonism. The involvement of the opioid system in delta 9-tetrahydrocannabinol-induced analgesia was investigated by using naloxone as well as delta (naltrindole)- and kappa (nor-binaltorphimine)-opioid receptor antagonists. Intrathecal nor-binaltorphimine antagonized the effect of delta 9-tetrahydrocannabinol. The effect of delta 9-tetrahydrocannabinol was also blocked by administration of dynorphin A-(1-8) antiserum in the same test.
Δ9-四氢大麻酚通过脊髓和脊髓上机制在啮齿动物中引发镇痛作用。药理学数据表明大麻素与阿片系统之间存在联系。缺乏特异性大麻素受体拮抗剂阻碍了对大麻素系统在痛觉控制中的生理相关性的研究。在这项工作中,我们表征了新型大麻素受体拮抗剂SR-141,716 A(N-哌啶基-5-(4-氯苯基)-1-(2,4-二氯苯基)-4-甲基-3-吡唑甲酰胺盐酸盐)对Δ9-四氢大麻酚诱导的镇痛作用的影响。在甩尾试验以及热板试验中的舔舐和跳跃反应中,pA2值分别为9.59、8.72和10.21。pA2图的斜率值与-1无差异,表明为竞争性拮抗作用。通过使用纳洛酮以及δ(纳曲吲哚)和κ(去甲双丙戊酰吗啡)阿片受体拮抗剂来研究阿片系统在Δ9-四氢大麻酚诱导的镇痛作用中的参与情况。鞘内注射去甲双丙戊酰吗啡可拮抗Δ9-四氢大麻酚的作用。在同一试验中,注射强啡肽A-(1-8)抗血清也可阻断Δ9-四氢大麻酚的作用。