Carruthers S G, Hosler J P, Pentikainen P, Azarnoff D L
Clin Pharmacol Ther. 1978 Aug;24(2):168-74. doi: 10.1002/cpt1978242168.
A Phase I evaluation of a new adrenoceptor blocker, pamatolol, was performed in 10 healthy male volunteers. Minor reductions in standing and exercise and isoproterenol-induced increases in heart rate were observed with the 10-mg oral dose and appeared maximal with the 400-600 mg dose. The rate of decline of effect averaged 1.5% of the exercise heart rate/hr. Neither resting systolic time intervals nor post-exercise pulmonary function was affected by this dose range of pamatolol. Based on the latter responses and the isoproterenol dose response curve, we tentatively conclude that pamatolol is relatively cardioselective in man.
对10名健康男性志愿者进行了新型肾上腺素能受体阻滞剂帕马洛尔的I期评估。口服10毫克剂量时，站立、运动及异丙肾上腺素诱发的心率增加略有降低，400 - 600毫克剂量时效果似乎最大。效应下降速率平均为运动心率的1.5%/小时。帕马洛尔的该剂量范围对静息收缩时间间期和运动后肺功能均无影响。基于后者的反应及异丙肾上腺素剂量反应曲线，我们初步得出结论，帕马洛尔在人体中具有相对心脏选择性。
