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目的 分析α1 肾上腺素受体阻断药多沙唑嗪手性对映体对兔胸主动脉和颈总动脉的选择性作用 ,以探讨作为良性前列腺增生症治疗药物的可能性。方法 测定去甲肾上腺素 (NE)诱发兔离体胸主动脉和颈总动脉收缩反应 ,并采用Schild作图法计算rac 多沙唑嗪、R 多沙唑嗪和S 多沙唑嗪的pA2 值。结果 在兔胸主动脉和颈总动脉 ,0 .0 3 ,0 .1和 0 .3μmol·L-1 的rac 多沙唑嗪、R 多沙唑嗪和S 多沙唑嗪均使NE诱发的血管收缩反应量效曲线平行右移 ,Emax不变 ;由Schild作图法计算得到的多沙唑嗪及其手性对映体的斜率值 ,经统计学分析符合竞争性拮抗。3种拮抗剂pA2 值的强度顺序为 :R 多沙唑嗪 >rac 多沙唑嗪 >S 多沙唑嗪。结论 与多沙唑嗪及其手性对映体对人前列腺组织作用的报道结果不同 ,S 多沙唑嗪对兔胸主动脉和颈总动脉α1 肾上腺素受体拮抗作用的选择性显著低于rac 多沙唑嗪和R 多沙唑嗪
OBJECTIVE: To analyze the selective effect of the doxazosin chiral enantiomers on the thoracic aorta and common carotid artery in rabbits in order to explore the possibility of treating the benign prostatic hyperplasia. Methods The contractile responses of isolated thoracic aorta and common carotid arteries in noradrenalin (NE) -related rats were measured. The pA2 values of rac doxazosin, R-doxazosin and S-doxazosin were calculated by Schild plot . Results In rabbits thoracic aorta and common carotid artery, rac doxazosin at 0. 03, 0. 1 and 0. 3 μmol·L-1, R-doxazosin and S doxazosin all induced NE-induced Vasoconstriction response of the dose-response curve parallel to the right shift, Emax unchanged; calculated by Schild plot slope of doxazosin and its chiral enantiomer, statistically consistent with competitive antagonism. The intensity order of the three antagonist pA2 values was: R doxazosin> rac doxazosin> S doxazosin. Conclusion The reported results of doxazosin and its chiral enantiomers on human prostate tissue are different. The selectivity of S-doxazosin on the α1-adrenergic receptors in the thoracic and common carotid arteries of rabbits is significantly lower than that of rac doxazosin and R doxazosin