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用大鼠离体胸主动脉环和豚鼠离体气管条功能实验及放射配基受体结合实验研究盐酸小檗碱(Ber)对组织毒蕈碱受体(M受体)的作用.结果表明较高浓度的Ber(≥20μmol·L-1)对有内皮的动脉环具直接舒张作用;在去内皮或阻断M受体后,其舒张作用被完全抑制.Ber使豚鼠离体气管条产生浓度依赖性收缩,此作用可被阿托品拮抗,其pA2值为9.8.放射配基受体结合实验显示,Ber对大鼠的唾液腺,大脑皮质和心脏M受体均有中度亲和力,且使[3H]-二苯羟乙酸奎宁酯(QNB)与3种组织M受体结合的Kd值增大,最大结合量不变.其Ki值分别为(7.6±1.3),(1.6±0.9)和(0.58±0.07)μmol·L-1.结果提示,Ber有M受体激动作用.
The effect of Berberine hydrochloride on muscarinic receptor (M receptor) was studied by the function of isolated tracheal strips in vitro and guinea pig tracheal strips and radioligand binding assay. The results showed that higher concentrations of Ber (≥20μmol·L-1) had direct relaxation on the endothelial artery rings. When the endothelium was blocked or the M receptor was blocked, its relaxation was completely inhibited. Ber induced a concentration-dependent contraction of guinea pig isolated tracheal strips, which was antagonized by atropine with a pA2 value of 9.8. Radioligand receptor binding experiments showed that Ber had moderate affinities to salivary gland, cerebral cortex and cardiac M receptor in rats, and the binding of [3H] -biphenylacetic acid quinine (QNB) with three kinds of tissue M Kd value of receptor binding increased, the maximum binding capacity unchanged. The Ki values were (7.6 ± 1.3), (1.6 ± 0.9) and (0.58 ± 0.07) μmol·L-1, respectively. The results suggest that Ber has M receptor agonism.