Coelho J, Schnelle K, Joubert L, Ventura D, Mullane J
Br J Clin Pharmacol. 1985 Apr;19(4):411-6. doi: 10.1111/j.1365-2125.1985.tb02663.x.
Cetamolol is a new beta-adrenoceptor blocking agent shown in animals to have moderate beta 1-adrenoceptor selectivity and partial agonist activity. In healthy normal volunteers, beta 1-adrenoceptor blockade was measured as the reduction of exercise-induced tachycardia, systolic blood pressure, and double product at 2, 8, and 24 h after a single oral dose of 10, 25, and 50 mg cetamolol. beta 1-adrenoceptor blockade was significantly linearly related to log serum cetamolol level, was maximal at 2 h, and was still clinically significant at 24 h. A crossover study of single 0, 10, and 25 mg doses confirmed these findings.
西他洛尔是一种新型β-肾上腺素能受体阻滞剂，在动物实验中显示具有中等程度的β1-肾上腺素能受体选择性和部分激动剂活性。在健康正常志愿者中，单次口服10、25和50毫克西他洛尔后，分别在2、8和24小时测量β1-肾上腺素能受体阻滞情况，以运动诱发的心动过速、收缩压和双乘积的降低来衡量。β1-肾上腺素能受体阻滞与血清西他洛尔水平的对数呈显著线性相关，在2小时时达到最大值，在24小时时仍具有临床意义。一项对0、10和25毫克单剂量的交叉研究证实了这些结果。
