纳曲酮与纳洛酮对吗啡，依托尼秦及羟甲芬太尼的拮抗作用比较

Comparison of the antagonistic effects of naltrexone and naloxone against morphine,etonitazene and ohmefentanyl

在整体和受体水平对阿片受体拮抗剂纳曲酮和纳洛酮对吗啡，依托尼秦和［３Ｈ］羟甲芬太尼的拮抗作用进行了比较．研究表明，在整体水平，纳曲酮在很小剂量下就能对抗吗啡在小鼠的镇痛作用，小鼠吗啡急性中毒以及依托尼秦致大鼠翻正反射消失．与纳洛酮相比，纳曲酮强效，长效，ｉｇ有效．受体水平纳曲酮抑制［３Ｈ］羟甲芬太尼与大鼠脑阿片受体结合的强度是纳洛酮的３．６倍，与整体水平实验结果一致。

Acompahson of the antagonistic ef-fects of naltrexone and naloxone against morpine,etonitazene and ohmefentanyl was studied.Naltrexoneeven at low dose had antagonistic effects on analgesiaproduced by morphine,acute intoxication caused bymorphine in mice and loss of righting reflex induced byetonitazene in rats.As compared with naloxone,naltrexone was effective by oral administration morepotent and with longduration. In preparation of ratbrain homogenates、the displacement of naltrexoneand naloxone on the binding of[3H] ohmefentanyl(predominantly μ receptor)was compared. The resultshowed that the potency of naltrexone was 3.6 timesthat of naloxone.