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实验以清醒大鼠的缩腿潜伏期为指标,观察了腹腔注射美普他酚及其同分异构体112824和112825对角叉菜胶引起的热痛敏的影响。外周炎症由单侧足底注射角叉菜胶(2mg/100μl)引起。注射角叉菜胶3h后,注射侧后肢局部红肿及热病过敏反应达到高峰,持续数小时。腹腔注射0.1mg/kg美普他酚对炎症和非炎症侧后肢的缩腿潜伏期无明显影响(P>0.05,n=8)。腹腔注射1mg/kg和10mg/kg美普他酚对炎症和非炎症侧后肢产生明显的抗痛敏和抗伤害效应,且对炎症侧缩腿反应的抑制(抗痛敏)作用明显强于非炎症侧(抗伤害)(P<0.05,n=8～11)。预先腹腔注射1.5mg/kg纳洛酮明显阻断美普他酚引起的抗伤害和抗痛敏效应。腹腔注射美普他酚的同分异构体112824(1mg/kg)和112825(1.5mg/kg)可产生与美普他酚类似的抗痛敏作用,该效应可被预先腹腔注射1.5mg/kg纳洛酮完全阻断。提示美普他酚及其同分异构体具有明显抗伤害和抗痛敏作用,且以后者为强。该作用主要通过mu阿片受体介导。本研究为扩展美普他酚及其同分异构体在临床上的应用提供了依据。
In the experiment, the latency of leg contraction in awake rats was used as an index to observe the effect of intraperitoneal injection of meptazinol and its isomers 112824 and 112825 on the thermal hyperalgesia induced by carrageenan. Peripheral inflammation was caused by unilateral plantar injection of carrageenan (2 mg / 100 μl). After injection of carrageenan for 3h, local hindlimb infiltration on the injection side and fever allergic reaction peaked for several hours. Intraperitoneal injection of 0.1 mg / kg meptazinol had no significant effect on the cul-de-sac latency of inflammatory and non-inflammatory hindlimbs (P> 0.05, n = 8). The intraperitoneal injection of 1 and 10 mg / kg meptazin had obvious anti-hyperalgesia and antinociceptive effects on inflammatory and non-inflammatory hindlimbs, and the inhibition (anti-hyperalgesia) on the side-shuffled inflammation was significantly stronger than non-inflammatory Side (anti-injury) (P <0.05, n = 8-11). Preperitoneal injection of naloxone at 1.5 mg / kg significantly blocked the anti-nociceptive and anti-nociceptive effects of meptazinol. Intraperitoneal injection of meptazinol isomers 112824 (1 mg / kg) and 112825 (1.5 mg / kg) produced an anti-hyperalgesia similar to that of meptazinol, which can be pre-ip injected with 1.5 mg / kg Naloxone completely blocked. Tip meptazinol and its isomers have obvious anti-injury and anti-hyperalgesia, and the latter is strong. This effect is mediated mainly by mu opioid receptors. This study provides the basis for expanding the clinical application of meptazinol and its isomers.