Clement J G, Copeman H T
Life Sci. 1984 Apr 9;34(15):1415-22. doi: 10.1016/0024-3205(84)90055-9.
Soman (50 micrograms/kg) and sarin (120 micrograms/kg), potent organophosphate anticholinesterase agents, produced an analgesic response in the mouse hotplate latency test. Naloxone antagonized but did not completely reverse the soman- and sarin-induced analgesia, whereas atropine antagonized completely the soman-and sarin-induced analgesia. Soman poisoning did not potentiate morphine-induced analgesia. It was simply an additive response. In survivors of soman (287 micrograms/kg) poisoning, the analgesia was more pronounced and was still apparent 96 hr after administration. This analgesia was completely antagonized by naloxone. Similar results were found in survivors of sarin (510 micrograms/kg) poisoning. The organophosphate-induced analgesia was not due to physical incapacitation as evidenced by performance on the accelerating rotorod. It is suggested that the organophosphate-induced analgesia is due to a combination of an increased concentration of acetylcholine due to inhibition of acetylcholinesterase combined with a reduced destruction of endogenous opioid-like substances due to organophosphate inhibition of proteases.
梭曼(50微克/千克)和沙林(120微克/千克)是强效有机磷酸酯类抗胆碱酯酶剂,在小鼠热板潜伏期试验中产生了镇痛反应。纳洛酮拮抗但未完全逆转梭曼和沙林诱导的镇痛作用,而阿托品则完全拮抗梭曼和沙林诱导的镇痛作用。梭曼中毒并未增强吗啡诱导的镇痛作用。这只是一种相加反应。在梭曼(287微克/千克)中毒的存活者中,镇痛作用更明显,给药后96小时仍很明显。这种镇痛作用被纳洛酮完全拮抗。在沙林(510微克/千克)中毒的存活者中也发现了类似结果。有机磷酸酯类诱导的镇痛作用并非由于身体机能丧失,加速转棒试验的表现证明了这一点。有人提出,有机磷酸酯类诱导的镇痛作用是由于乙酰胆碱酯酶受抑制导致乙酰胆碱浓度增加,以及有机磷酸酯类抑制蛋白酶导致内源性阿片样物质破坏减少共同作用的结果。