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我们设计和合成了一个新的亲和标记配基:7α-二(β-氯乙基)胺基-6,14-乙烯撑基-四氢奥利文(简称α-CAO)。镇痛试验表明它的活性为吗啡的2～7倍,并具有作用时间长和毒性低等优点。经抑制豚鼠回肠纵肌(GPI)和小鼠输精管(MVD)收缩试验以及大鼠脑(去小脑)P_2膜制备的亲和力试验,发现其分别是吗啡的3、12和21倍,通过洗涤和纳洛酮反转试验证实α-CAO为阿片受点不可逆结合的激动剂。
We designed and synthesized a new affinity tagged ligand: 7α-bis (β-chloroethyl) amino-6,14-vinylene-tetrahydropurin (a-CAO). Analgesic test showed that its activity is 2 to 7 times that of morphine, and has the advantages of long duration of action and low toxicity. The inhibitory effect on the contraction of guinea pig ileum longitudinal muscle (MIP) and mouse vas deferens (MVD) and the preparation of P_2 membrane in rat brain (to the cerebellum) were found to be 3, 12 and 21 times that of morphine, respectively. The reversal test of losartan confirmed that α-CAO is an agonist of opioid irreversible binding.