摘要
α-CAM是一新的阿片受点不可逆激动剂,在离体组织(GPI,MVD,RVD和RbVD)及大鼠脑P_2膜制备上均表现不可逆作用。对小鼠镇痛(icv)ED_(50)为0.12 nmol/鼠,镇痛作用可持续2～3 d,是迄今所知镇痛时间最长的化合物。一次注射(icv)即可使小鼠成瘾,可作为研究成瘾机理的工具药。
7α-bis (β-chloroethyl) aminomethyl-6, 14-endoetheno-tetrahydro oripavine (a-CAM) is a new irreversible opioid receptor agonist. Its effect on isolated tissues (guinea pig ileum, mouse vas deferens, rat vas deferens and rabbit vas deferens) were studied. It was shown to be bound irreversibly to rat brain P_2 membrane preparations. The ED_(50) of its analgesic effect in mice (icy) was found to be 0.12 nmol/mouse, and the effect may last as long as 2～3 days. It is a compound which produces the longest analgesia known up to date. A single dose (icy) of a-CAM was sufficient to produce dependence in mice. Thus, the compound may serve as an agent for studying the mechanism of physical dependence.
出处
《药学学报》
CAS
CSCD
北大核心
1989年第5期321-325,共5页
Acta Pharmaceutica Sinica
基金
国家自然科学基金
关键词
阿片受点
不可逆激动剂
药理研究
Opioid receptors
Irreversible agonist
7α-bis (β-chloroethyl) aminomethyl-6, 14-endothenotetrahydrooripavine (α-CAM)
Analgesic
Dependence
