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本文证明小檗碱(Ber)具有阻滞α肾上腺素受体的作用。Ber能竞争性拮抗苯福林所致大鼠肛尾肌和兔主动脉条的收缩反应,pA_2值分别为6.62及6.54。对大鼠输精管,Ber能使可乐定的量效曲线平行右移,最大反应不变,其pA_2值为5.3。对毁脊髓大鼠,Ber能竞争性拮抗甲氧明升高舒张压的作用。放射配体结合试验证明Ber对α_1和α_2受体有亲和力,其表观解离常数(Ki)分别为1.78μmol/L和0.47μmol/L。对清醒大鼠,Ber能增强心肌收缩性,降低血压,且降低舒张压甚于降低收缩压。
This paper proves that berberine has the effect of blocking alpha adrenergic receptor. Ber competitively antagonized phenylephrine-induced contractile responses in the rostral and rabbit aortic strips of rats, with pA values of 6.62 and 6.54, respectively. For rat vas deferens, Ber can make the dose-response curve of clonidine move to the right parallel, the maximum response unchanged, the pA_2 value of 5.3. On the destruction of spinal cord rats, Ber can competitively antagonize the role of methylamine in increasing diastolic blood pressure. Radioligand binding assays demonstrated that Ber has an affinity for alpha 1 and alpha 2 receptors with an apparent dissociation constant (Ki) of 1.78 and 0.47 μmol / L, respectively. In conscious rats, Ber can enhance myocardial contractility, lower blood pressure, and lower diastolic pressure than systolic blood pressure.