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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。
OBJECTIVE: To observe the effect of naftopidil derivative BWYJ on blood pressure and hemodynamics in hypertensive rats and normal rats. Methods: Hypertension and normal rats were given intravenous and intragastric administration respectively, the change of blood pressure was observed, the hemodynamics of the cat was measured by anesthesia and thoracotomy, and the neuromuscular specimens Buck mechanism. Results BWYJ1.2 and 2.4 mg · kg-1iv decreased systolic pressure (SAP) and diastolic pressure (DAP) in normal and hypertensive rats, and the effect was prolonged with the increase of dose. BWYJ at doses of 10, 20 and 40 mg · kg-1, respectively, decreased SAP (maximum effect decreased 4.6%, 13.0%, 16.8%) and DAP (decreased 7.1%, 17.9%, 20.5% After recovery. Compared with normal rats, BWYJ at 5, 10 and 20 mg · kg-1 significantly decreased SAP (7.3%, 16.5%, 20.4%) and DAP (8.5%, 14.8%, 24.5% Significantly longer. Twelve rectal administrations of anesthetized cats resulted in the decrease of DAP and LVWI in BWYJ2.5mg · kg-1 and the decrease of SAP, DAP, TPR, ± dp / dtmax and LVWI in BWYJ5mg · kg-1. Conclusion: Intravenous or intragastric administration of BWYJ can depress the blood pressure in normal and renal hypertensive rats. The antihypertensive effect is independent of central and ganglia.