Dibona G F, Sawin L L
J Pharmacol Exp Ther. 1984 Feb;228(2):420-4.
The renal tubular site of action of felodipine was localized using renal clearance and recollection micropuncture techniques in the anesthetized rat. In initial renal clearance experiments, felodipine (2.75 nM/kg/min i.v. X 60 min) had no effect on mean arterial pressure or glomerular filtration but significantly increased urinary flow rate, sodium and potassium excretion. In subsequent recollection micropuncture experiments, felodipine decreased mean arterial pressure but did not affect renal blood flow or renal vascular resistance or glomerular filtration rate; absolute and fractional urinary excretion of sodium and water, but not potassium, were increased. Proximal tubular and loop of Henle sodium, potassium and water reabsorption were not affected but distal tubular and collecting duct sodium and water (not potassium) reabsorption were decreased by felodipine. Felodipine is a vasodilator antihypertensive agent which, in doses which decrease mean arterial pressure in normotensive rats, increases urinary flow rate and sodium excretion by inhibiting distal tubular and collecting duct sodium and water reabsorption; potassium reabsorption or excretion is not affected. As a vasodilator antihypertensive agent, felodipine possesses beneficial natriuretic rather than detrimental sodium retaining properties.
在麻醉大鼠中,采用肾清除率和逆向微穿刺技术确定了非洛地平的肾小管作用部位。在最初的肾清除率实验中,非洛地平(静脉注射2.75 nM/kg/分钟,共60分钟)对平均动脉压或肾小球滤过无影响,但显著增加尿流率、钠和钾排泄。在随后的逆向微穿刺实验中,非洛地平降低了平均动脉压,但不影响肾血流量、肾血管阻力或肾小球滤过率;钠和水的绝对及分数排泄增加,但钾排泄未受影响。非洛地平不影响近端小管和髓袢的钠、钾及水重吸收,但可减少远端小管和集合管的钠和水(而非钾)重吸收。非洛地平是一种血管扩张性抗高血压药物,在能降低正常血压大鼠平均动脉压的剂量下,通过抑制远端小管和集合管的钠和水重吸收来增加尿流率及钠排泄;钾重吸收或排泄不受影响。作为一种血管扩张性抗高血压药物,非洛地平具有有益的利钠作用,而非有害的保钠作用。