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一、概况 盐酸纳洛酮(Naloxonc Hy-drochloride、商品名Narcan)合成于1960年,为羟(二)氢吗啡酮衍生物。1961年Blumberg等报道了纳洛酮能拮抗羟(二)氢吗啡酮引起的小鼠镇痛、致死和兔的呼吸抑制作用,较烯丙吗啡(Nalorphine)强7—10倍,1963年Foldcs在人体观察纳洛酮对麻醉镇痛药的拮抗作用。纳洛酮是阿片受体的拮抗剂,临床用于麻醉镇痛药的过量和中毒的治疗。基础方面用于对阿片受体、内源性阿片样物质和镇痛药作用机理等的研究。在
I. Overview Naloxonc hydrochloride (Naloxonc Hy-drochloride, trade name Narcan) was synthesized in 1960, for hydroxy (di) hydromorphone derivatives. 1961 Blumberg et al reported that naloxone can antagonize the hydromorphone induced analgesia in mice, lethal and respiratory depression in rabbits, 7-10 times stronger than almorphine (Nalorphine), Foldcs in 1963 Observation on the Antagonism of Naloxone to Narcotic Analgesic in Human Body. Naloxone is an antagonist of opioid receptors and is used clinically for the treatment of overdose and poisoning of narcotic analgesics. Fundamentals are used to study the mechanisms of action of opioid receptors, endogenous opioids and analgesics. in