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用放射受体结合方法,研究了36种四氢异喹啉类生物碱及其半合成衍生物对大鼠脑内M-胆碱受体的结合特性。实验发现,粉防己碱对M-胆碱受体的亲和力最高,其K_i值为7.3×10~(-8)mol/L。小檗胺、四氢黄连碱和半合成原小檗碱衍生物B_1亦具有较高亲和力,K_i值分别为1.9×10~(-7),6.8×10~(-7)和8.1×10~(-7)mol/L。四氢小檗碱半合成原小檗碱衍生物B_2,B_3,B_4,B_5,B_6和半合成小檗胺衍生物E_1及半合成蝙蝠葛碱衍生物D_1对M-胆碱受体的亲和力为中等强度,K_i值在1～2×10~(-6)mol/L之间。实验结果提示,某些四氢异喹啉类生物碱的药理作用可能与M-胆碱受体有关。
The binding properties of 36 tetrahydroisoquinoline alkaloids and their semisynthetic derivatives to M-choline receptors in rat brain were studied by radioactive receptor binding. It was found that tetrandrine had the highest affinity to M-choline receptor with a K_i value of 7.3 × 10 -8 mol / L. Berbamine, tetrahydropiperazine and semi-synthetic protoberberine derivatives B_1 also had higher affinity with K_i values of 1.9 × 10 -7, 6.8 × 10 -7 and 8.1 × 10 -7, (-7) mol / L. The affinity of tetrahydrobiopterin derivatives of Berberine B_2, B_3, B_4, B_5, B_6 and semicompound berbamine derivatives E_1 and the hemidesynthetic attarium derivative D_1 to M-choline receptors were Medium intensity, K_i value between 1 ~ 2 × 10 -6 mol / L. The experimental results suggest that some of the tetrahydroisoquinoline alkaloids pharmacological effects may be related to M-choline receptors.