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P—7521盐酸盐经溴化后,进行催化卤氚置换反应,得到>95％放化纯度的[~3H]P—7521。[~3H]P—7521可高亲和地结合大鼠脑P_2膜阿片受体,其K_(D1)和K_(D2)分别为0.030和0.75nmol/L。Na~+对[~3H]P—7521的特异结合无影响。[~3H]P—7521与阿片受体结合后的解离研究表明:约50％的结合在20min内很快解离,剩余的50％则解离极慢,4h时仍有35％的结合存在。[~3H]P—7521结合的膜经4次洗涤仍可测得对照组的87％的结合。[~3H]P—7521与阿片受体的结合是很牢固的。
After the P-7521 hydrochloride was brominated, the catalytic halogen tritium exchange reaction was carried out to obtain [~ 3H] P-7521 with a radiochemical purity of> 95%. [~ 3H] P-7521 could bind with high affinity to P_2 opioid receptor in rat brain with K_ (D1) and K_ (D2) values of 0.030 and 0.75 nmol / L, respectively. Na ~ + had no effect on the specific binding of [~ 3H] P-7521. Dissociation studies of [~ 3H] P-7521 binding to opioid receptors showed that about 50% of the binding dissociated rapidly within 20 min and the remaining 50% dissociated very slowly with 35% binding still at 4 h exist. The [~ 3H] P-7521-bound membrane still measured 87% of the controls in the control group after 4 washes. The binding of [~ 3H] P-7521 to opioid receptors is very robust.