ICI 66,082对人体心脏和肺部β-肾上腺素能受体阻断活性的研究。
An investigation into the cardiac and pulmonary beta-adrenoceptor blocking activity of ICI 66,082 in man.
作者信息
Marlin G E, Kumana C R, Kaye C M, Smith D M, Turner P
出版信息
Br J Clin Pharmacol. 1975 Apr;2(2):151-7. doi: 10.1111/j.1365-2125.1975.tb01570.x.
Abstract
1 Oral ICI 66,082 (200 mg) or water (control treatment) were each administered to six healthy volunteers. 2 The heart rate (HR) and peak flow rate (PFR) were measured at rest and during vigorous exercise before and at intervals up to 24 h after each treatment. 3 ICI 66,082 produced significant reductions in exercise HR at all times compared with the changes after the control treatment (P less than 0.001), whereas with resting HR, corresponding significant reductions only occurred at 2,3 and 4 h (P less than 0.05). 4 Although there was no change in resting PFR, significant reductions in exercise PFR, compared with the changes after the control treatment, occurred at all times excepting at 2 h after ICI 66,082 (P less than 0.025). 5 The findings are consistent with ICI 66,082 possessing partial cardioselectivity. 6 Plasma levels and renal excretion of the drug were determined. Urinary recovery was variable which, together with the plasma concentration/effect relationships obtained, raise the possibility that ICI 66,082 is metabolized in man.
摘要
给6名健康志愿者分别口服ICI 66,082（200毫克）或水（对照处理）。
在每次处理前及处理后直至24小时的间隔时间内，于静息状态和剧烈运动时测量心率（HR）和峰值流速（PFR）。
与对照处理后的变化相比，ICI 66,082在所有时间均使运动心率显著降低（P<0.001），而静息心率仅在2、3和4小时出现相应的显著降低（P<0.05）。
尽管静息PFR没有变化，但与对照处理后的变化相比，除ICI 66,082给药后2小时外，运动PFR在所有时间均显著降低（P<0.025）。
这些发现与ICI 66,082具有部分心脏选择性一致。
测定了药物的血浆水平和肾排泄情况。尿回收率各不相同，结合所获得的血浆浓度/效应关系，提示ICI 66,082在人体内可能会被代谢。
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