Knoll J, Fürst S, Makleit S
J Pharm Pharmacol. 1975 Feb;27(2):99-105. doi: 10.1111/j.2042-7158.1975.tb09416.x.
6-Deoxy-6-dihydroazido-14-hydroxyisomorphine (14-hydroxyazidomorphine) was synthesized, its analgesic potency in mice and rats, its antitussive effect in rats and its dependence liability in mice, rats and monkeys were studied. Azidomorphine the 14-nonhydroxylated parent molecule, morphine, hydromorphone and oxymorphone were used for comparison. 14-Hdroxyazidomorphine proved to be as potent an analgesic as azidomorphine, even more potent as an antitussive, and showed the same low tolerance and dependence capacity. It was 11-6 times less toxic than azidomorphine in mice and 6-5 times less toxic in rats.
合成了6-脱氧-6-二氢叠氮基-14-羟基异吗啡酮（14-羟基叠氮吗啡），并研究了其在小鼠和大鼠中的镇痛效力、在大鼠中的镇咳作用以及在小鼠、大鼠和猴子中的成瘾倾向。将叠氮吗啡（14-未羟基化的母体分子）、吗啡、氢吗啡酮和羟吗啡酮用作对照。结果表明，14-羟基叠氮吗啡的镇痛效力与叠氮吗啡相当，镇咳作用甚至更强，且耐受性和成瘾性相同。其在小鼠中的毒性比叠氮吗啡低11-6倍，在大鼠中低6-5倍。
