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目的在动物疼痛模型上,观察泰国眼镜蛇长链突触后α-神经毒素cobratoxin (CTX)的化学修饰物receptin(REC)的镇痛作用及其阿托品和纳洛酮对其镇痛作用的影响。方法采用腹腔注射(i.p., 5 mg/kg, 7.07 mg/kg, 10mg/kg)或脑室注射(i.c.v., 62.5 g/kg)的方法给予REC;采用小鼠热板反应、扭体反应及大鼠甩尾反应试验研究药物的镇痛作用; 应用预先给予阿托品(atropine, Atr; 0.5 mg/kg, i.m. 或 10 mg/kg, i.p.)或纳洛酮(naloxone, Nal; 3 mg/kg,i.p.)研究胆碱能及阿片肽能神经在REC镇痛中的作用;采用Animex试验观察REC对小鼠自发活动的影响。结果REC(5 mg/kg,7.07 mg/kg及 10 mg/kg, i.p.)在小鼠热板试验及扭体试验中均呈现出剂量依赖性镇痛作用,并于给药后2~3 小时出现显著镇痛作用。在大鼠甩尾试验中,REC 62.5 mg/kg (相当于全身给药的1/160, i.c.v.)后产生显著镇痛作用。阿托品或纳洛酮不能阻断REC的镇痛作用。高剂量REC (10 mg/kg, i.p.)对小鼠的自发活动无明显影响。结论REC具有镇痛作用,尽管中枢神经系统参与REC的镇痛作用,但外周神经系统可能亦介导REC的镇痛作用。中枢胆碱能及阿片肽能神经系统可能不参与REC的镇痛作用。
Objective To investigate the analgesic effect of a receptor (REC), a chemical modification of long-chain synaptic α-neurotoxin cobratoxin (CTX), on the analgesic effect of atropine and naloxone in animal models of pain. Methods REC was given intraperitoneally (ip, 5 mg / kg, 7.07 mg / kg, 10 mg / kg) or intraventricular injection (icv, 62.5 g / kg) Drift test was used to study the analgesic effect of the drug. Atropine (Atr; 0.5 mg / kg, im or 10 mg / kg, ip) or naloxone (Nal; 3 mg / kg, ip) To study the role of cholinergic and opioid peptides in the analgesia of REC. To investigate the effect of REC on spontaneous activity in mice by using Animex test. Results REC (5 mg / kg, 7.07 mg / kg and 10 mg / kg, ip) showed a dose-dependent analgesic effect in hot-plate test and writhing test in mice, and after 2 to 3 hours A significant analgesic effect. REC 62.5 mg / kg (equivalent to 1/160, i.c.v. administered systemically) produced a significant analgesic effect in the rat tail flick test. Atropine or naloxone can not block the analgesic effect of REC. High-dose REC (10 mg / kg, i.p.) had no significant effect on spontaneous activity in mice. Conclusions REC has analgesic effect. Although central nervous system participates in the analgesic effect of REC, peripheral nervous system may also mediate the analgesic effect of REC. Central cholinergic and opioid nervous system may not participate in the analgesic effect of REC.