Petrov V E
Farmakol Toksikol. 1987 Mar-Apr;50(2):23-6.
At intrathecal administration the antinociceptive effect of morphine and DADL significantly exceeds the antinociceptive effect of pentazocine (ED50 in tail flick test were 1.1, 1.64, 75.0 nmol per mouse and in "writhing" test 0.0064, 0.0047, 24.53 nmol per mouse, respectively). All the agonists tested exhibited significantly higher activity at chemical stimulation than at thermal one. During the analysis of pA2 of naloxone during the interaction with morphine, DADL and pentazocine under thermal and chemical stimulation a pronounced mu-receptor component in the effect of DADL and pentazocine was suggested. A preliminary subcutaneous injection of sodium oxybutyrate (150 mg/kg) fails to change the activity of opioids administered intrathecally. Diazepam (5 mg/kg, subcutaneously) enhances the antinociceptive activity of DADL only at chemical stimulation. Haloperidol (2 mg/kg) increases the antinociceptive effect of morphine and DADL at pain stimulation of both types but exerts no influence on the analgesic effect of pentazocine. Haloperidol produces the most pronounced enhancement of the spinal component of delta-agonist DADL antinociceptive action. The enhancing effect of haloperidol is realized at the supraspinal level.
鞘内给药时,吗啡和DADL的抗伤害感受作用显著超过喷他佐辛的抗伤害感受作用(在甩尾试验中,每只小鼠的ED50分别为1.1、1.64、75.0纳摩尔,在“扭体”试验中,每只小鼠分别为0.0064、0.0047、24.53纳摩尔)。所有测试的激动剂在化学刺激下的活性均显著高于热刺激下的活性。在分析纳洛酮与吗啡、DADL和喷他佐辛在热刺激和化学刺激下相互作用时的pA2时,提示DADL和喷他佐辛的作用中存在明显的μ受体成分。预先皮下注射羟丁酸钠(150毫克/千克)不会改变鞘内给药的阿片类药物的活性。地西泮(5毫克/千克,皮下注射)仅在化学刺激时增强DADL的抗伤害感受活性。氟哌啶醇(2毫克/千克)在两种类型的疼痛刺激下均增加吗啡和DADL的抗伤害感受作用,但对喷他佐辛的镇痛作用无影响。氟哌啶醇对δ激动剂DADL抗伤害感受作用的脊髓成分产生最明显的增强作用。氟哌啶醇的增强作用是在脊髓上水平实现的。