摘要
在大鼠吗啡躯体依赖模型上,对纳美芬的拮抗效应进行了评价并在大鼠脑匀浆P2 膜上 ,观察了纳美芬对3H -NAL(主要为μ 受体)的抑制强度。结果表明,纳美芬0.25 -2.0mg·kg-1 可明显降低大鼠纳洛酮催促后的体重减轻,使大鼠跳跃、湿抖和激惹的发生率以及戒断症状综合记分明显低于吗啡对照组 ,纳美芬对吗啡所致大鼠的躯体依赖有较好的拮抗作用 ;纳美芬对3H -NAL竞争抑制的IC50 值为5.6×10-9 mol·L-1,与纳曲酮和纳洛酮的比值约为1∶1.2∶3.5 。
The effects of nalmefene on physical dependence induced by morphine in rats were evaluated and in P2 preparation of rat brain homogenates.The displacement of nalmefene on the binding of 3H-naloxone(predominantly μ-receptor) was studied. The results showed that nalmefene, with the dose of 0.2-0.5 mg·kg-1, could signicantly decrease the body weight loss of rats precipitated by naloxone. The incidence(%) of jumping, wet-dog shakes and irritability and the scores of the abstinence syndrome also significantly reduced compared with those of morphine group. The IC50 value of nalmefene against the binding of 3H-naloxone was 5.6×10-9 mol·L-1 and the proportion, nalmefene:naltrexone:naloxone, was about 1:1.2:3.5. Those results are basically in an agreement with their efficacies against morphine in rats.
出处
《中国药物依赖性杂志》
CAS
CSCD
2000年第1期14-16,共3页
Chinese Journal of Drug Dependence
关键词
纳美芬
吗啡
躯体依赖
阿片受体
nalmefene
morphine
physical dependence
opioid receptor
