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本实验表明苄基四氢巴马汀(BTHP)具有阻断α-肾上腺素受体的作用。它能竞争性拮抗苯肾上腺素所致大鼠肛尾肌和兔主动脉条的收缩反应,其pA_2值分别为5.86和5.8;也能浓度依赖性地使可乐定和B-HT920的量效曲线平行右移,最大反应不变,其pA_2值分别为5.2和5.3。放射配基结合测定表明,BTHP对α_1和α_2受体均有亲和力,其竞争抑制常数(K_i)分别为3.52μmol/L和8.1μmol/L。
This experiment shows that benzyl tetrahydropalmatine (BTHP) has the effect of blocking the α-adrenergic receptor. It competitively antagonized the phenylephrine-induced contractile response in the rostral and rabbit aortic strips of rats with pA_2 values of 5.86 and 5.8, respectively; and also dose-dependently enabled the clonidine and B-HT920 dose-response curves Parallel to the right shift, the maximum response unchanged, the pA_2 values were 5.2 and 5.3. Radioligand binding assay showed that BTHP had affinity to both α_1 and α_2 receptors, and its competitive inhibition constants (K_i) were 3.52μmol / L and 8.1μmol / L, respectively.