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本文比较了从中国萝芙木中提出的盐析碱spegatrine(SP) 及其双聚体dispegatrine(DISP)对α_1和α_2受体亲和力及其效应的影响。结果发现SP和DISP对α受体有亲和力,DISP的作用比SP强一个数量级。DISP对NE引起肛尾肌收缩呈拮抗作用,SP对小剂量NE呈抑制作用,对较大剂量NE表现协同作用,DISP和SP对可乐宁抑制输精管收缩均呈拮抗作用,DISP比SP强3~4倍。表明DISP为非选择性的α受体阻滞剂,而SP为α_2受体阳滞剂,对α_1受体作用性质尚待阐明。
In this paper, we compared the effects of salt-spelling spegatrine (SP) and dispegatrine (DISP) on the affinity of alpha 1 and alpha 2 receptors and their effects. As a result, it was found that SP and DISP have an affinity for α receptor, and DISP is an order of magnitude stronger than SP. DISP antagonized the contractile activity of NE caused by NE, SP inhibited NE and showed antagonistic effects on the contraction of vas deferens. DISP and SP showed antagonistic effects on the inhibition of vasoconstriction. DISP was 3 ~ 4 times. DISP is a non-selective α-blocker, while SP is an α-2 receptor blocker. The nature of action on the α-1 receptor remains to be elucidated.