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1960年Fishman 首先合成了纳洛酮(N-Allylynorexy Morphone;Naloxone 缩写N_x)。其结构虽似吗啡,但不成瘾,故不属麻醉药物禁限范围。N_x与具有双向激动-拮抗作用的药物如烯丙甲吗啡(Nalorphin);丙烯左吗喃(Levallorphan)和镇痛新(Pentazocine)等不同,N_x只具有拮抗中枢性麻醉药的作用。它极易通过血脑屏障,能较快地与内源性μ、K和σ三种阿片受体起竞争性拮抗作用,其中与μ受体亲合力最强。1961年Blumberg 报导N_x对镇痛有拮抗作用。近年来由于镇痛原理的研
In 1960, Fishman synthesized N-Allylynorexy Morphone (N_ox). Although its structure is like morphine, but not addiction, it does not belong to the restricted range of narcotic drugs. N_x is different from drugs with bidirectional agonistic-antagonistic actions such as Nalorphin, Levallorphan, Pentazocine, etc., and Nx has only antagonistic effects on central anesthetics. It easily cross the blood-brain barrier and rapidly compete with endogenous μ, K, and σ opioid receptors, with the highest affinity for μ receptor. Blumberg 1961 reported that N_x has analgesic antagonism. In recent years due to the principle of analgesia