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Chiral selective effects of doxazosin and its enantiomers on...

Chiral selective effects of doxazosin and its enantiomers on blood pressure and bladder vesical pressure in anesthetized rats

作     者:Ren Lei - ming . Ma Shi - ping. Zhao Ding. Lu Hai - gang. Department of Pharmacology. School of Pharmacy. Hebei Medical University. Shijiazhuang 050017 China 

会议名称:《第十五届国际药理学大会》

会议日期:1000年

学科分类:1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 100706[医学-药理学] 100602[医学-中西医结合临床] 10[医学] 

摘      要:正 Objective: To study chiral selective effects of doxazosin enantiomers on blood pressure and bladder vesical pressure in anesthetized rats. Method: In anesthetized rats, carotid blood pressure, left ventricular pressure of the heart and the vesical pressure of the bladder were recorded. Results: Administration of S - doxazosin at0.25. 2.5. 25 and 250nmol/kg iv produced a dose- dependent decrease in blood pressure, but its depressor effect was significantly weaker than that induced by R - doxazosin and racemin - doxazosin (rac - doxazosin). and the ED50 values of R - doxazosin. S - doxazosin and rac - doxazosin were 15.64. 45.93 and 128.81. respectively, rac- Doxazosin and its enantiomers administered accumulatively in anesthetized rats induced a dose - dependent decrease in the left ventricular systolic pressure (LVSP) and±dp/dtmax. and a potency order of the three agents was R - doxazosin rac - doxazosin S - doxazosin. rac - Doxazosin and its enantiomers decreased the vesical micturation pressure dose - de-pendently at 2.5. 25 and 250 nmol/kg. and the inhibitory potency among the three agents was same. Conclusion: S - doxazosin has chiral selectivity between cardiovascular system and urinary system in anesthetized rats.

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