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作 者:眭玉霞[1] 孙安盛[1] 吴芹[1] 余丽梅[1] 黄燮南[1] 石京山[1] 袁牧[2]
机构地区:[1]遵义医学院药理教研室 [2]贵州省中国科学院天然产物化学重点实验室
出 处:《中国临床药理学与治疗学》2005年第8期852-856,共5页Chinese Journal of Clinical Pharmacology and Therapeutics
基 金:国家自然科学基金资助项目(№30060087)
摘 要:目的:观察萘哌地尔衍生物BWYJ对高血压模型和正常大鼠血压及猫血流动力学的影响。方法:分别对高血压和正常大鼠静脉及灌胃给药,观察血压变化;利用麻醉开胸测定猫血流动力学的变化;采用侧脑室给药、猫在体瞬膜神经肌肉标本初步探讨降压机制。结果:BWYJ1.2及2.4mg·kg-1iv,降低正常及高血压大鼠收缩压(SAP)和舒张压(DAP),且随剂量的增加效应增加,作用时间延长。BWYJ10、20及40mg·kg-1灌胃给药,降低清醒正常大鼠SAP(最大效应分别下降4.6%、13.0%、16.8%)和DAP(分别下降7.1%、17.9%、20.5%),3h后恢复。BWYJ5、10及20mg·kg-1灌胃清醒高血压大鼠,降低SAP(下降7.3%、16.5%、20.4%)和DAP(8.5%、14.8%、24.5%),强于正常大鼠且时间明显延长。麻醉猫十二直肠给药,BWYJ2.5mg·kg-1仅DAP、LVWI降低,BWYJ5mg·kg-1使SAP、DAP、TPR、±dp/dtmax及LVWI明显降低,其他无明显变化。结论:BWYJ静脉或灌胃给药对正常和肾性高血压大鼠产生降压作用,降压作用与中枢、神经节无关。AIM: To observe the effects of BWYJ on blood pressure (BP) in the normal-tensive, hypertensive rats and haemodynamics in cats. METHODS: The BP of the normal-tensive and renal hypertensive rats was measured and hemodynamics parameters were recorded in thoractomic cats. The effects of BWYJ on cardiovaseular center and ganglia were observed. RESULTS: In normaltensive and hypertensive rats, BWYJ of 1.2 and 2.4 mg·kg^-1 (iv) decreased SAP and DAP in normal-tension rats. BWYJ at oral doses of 10, 20 and 40 mg·kg^-1 had a hypotensiove effect with little influence in heart rate. In hypertensive rats, the hypotensive effect of BWYJ were in a dose-dependent manner at oral doses of 5, 10 and 20 mg·kg^-1 . BWYJ 2.5 mg·kg^-1 by duodenum produced areduction of DAP, TPR and LVWI. BWYJ 5.0 mg·kg^-1 produced a reduction of SAP, DAP, LVSP, ± dp/dtmax and TPR. The drop in BP was not observed by icy BWYJ. The contraction of third eyelid induced by the stimulation of preganglionic fibre of superior cervical nerve ganglia was not effected by BWYJ. CONCLUSION: BWYJ may decrease the blood pressure in the renal hypertensive and normal-tensive rats. The hypotensive effect of BWYJ is mainly due to vasodilating and declining perpheral resistance, and the inhibition of myocardial contractility might play a hypotensive role.
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