Gennari C, Pollavini G, Nami R, Francini G, Bianchini C, Verdecchia P
Eur J Clin Pharmacol. 1984;26(6):695-8. doi: 10.1007/BF00541927.
In a randomised within-subject double-blind study, 7 healthy male volunteers, aged 32 to 40 years, received at rest intravenous infusions of 2 mg propranolol (devoid of partial agonist activity), 2 mg oxprenolol (with partial agonist activity) and placebo. Cuff blood pressure did not vary after any of the 3 treatments. The heart rate did not change after placebo, but fell in the first 5 min both after propranolol and oxprenolol (p less than 0.01); the rate was slightly lower after propranolol than oxprenolol (p less than 0.05). The heart rate remained lower after both beta-blockers than placebo from 5 to 60 min after the infusion (both p less than 0.01), but the difference between the two beta-blockers was no longer significant. Plasma cyclic AMP showed a peak rise at 2 and 3 min after oxprenolol, and remained unchanged at those times after propranolol and placebo. From the 5th to the 60th min after infusion, the cyclic AMP concentration was lower after both beta-blockers than placebo, and with a slightly but not significantly higher level on oxprenolol than propranolol. Plasma noradrenaline and adrenaline were higher after the beta-blockers compared to placebo. Oxprenolol evoked a smaller and non-significant rise in both catecholamines. That oxprenolol, unlike propranolol, causes a sudden rise in plasma cyclic AMP soon after an i.v. infusion may be due to its partial agonist activity.
在一项随机、受试者自身对照的双盲研究中，7名年龄在32至40岁之间的健康男性志愿者在静息状态下接受了静脉输注，分别为2毫克普萘洛尔（无部分激动剂活性）、2毫克氧烯洛尔（有部分激动剂活性）和安慰剂。三种治疗中的任何一种后，袖带血压均无变化。安慰剂治疗后心率未改变，但普萘洛尔和氧烯洛尔治疗后最初5分钟内心率均下降（p<0.01）；普萘洛尔治疗后的心率略低于氧烯洛尔（p<0.05）。输注后5至60分钟内，两种β受体阻滞剂治疗后的心率均低于安慰剂（均p<0.01），但两种β受体阻滞剂之间的差异不再显著。血浆环磷酸腺苷（cAMP）在氧烯洛尔输注后2至3分钟出现峰值升高，而在普萘洛尔和安慰剂输注后相同时间保持不变。输注后第5至60分钟，两种β受体阻滞剂治疗后的环磷酸腺苷浓度均低于安慰剂，且氧烯洛尔的浓度略高于普萘洛尔，但差异不显著。与安慰剂相比，β受体阻滞剂治疗后血浆去甲肾上腺素和肾上腺素水平升高。氧烯洛尔引起的两种儿茶酚胺升高幅度较小且无统计学意义。与普萘洛尔不同，氧烯洛尔静脉输注后不久会导致血浆环磷酸腺苷突然升高，这可能归因于其部分激动剂活性。
