Mann W S, Sales E F, Van Inwegen R G, Barrett J A, Smith R D, Wolf P S
Arch Int Pharmacodyn Ther. 1986 Nov;284(1):53-71.
Studies were conducted to evaluate the effects of celiprolol on alpha-adrenergic stimulation of dog saphenous vein rings (postsynaptic effect) and on catecholamine outflow from the dog coronary circulation during sympathetic nerve stimulation in vivo (presynaptic effect). In venous rings, celiprolol, 10(-6) to 10(-4) M, shifted the concentration-response curve to BHT 920 in a concentration-related manner, but had no effect on the response to methoxamine at concentrations less than 10(-4) M. During continuous stimulation of the right stellate ganglion, celiprolol, 1-10 mg/kg i.v., increased the catecholamine concentration in the coronary sinus, while decreasing heart rate. In contrast, propranolol did not affect catecholamine concentration but decreased heart rate, rauwolscine increased both catecholamine concentration and heart rate, and clonidine decreased both catecholamine concentration and heart rate. These results are consistent with the hypothesis that celiprolol possesses weak alpha 2-antagonist properties in addition to its beta 1-blocking activity.
开展了多项研究，以评估塞利洛尔对犬隐静脉环α-肾上腺素能刺激的影响（突触后效应），以及对犬在体交感神经刺激期间冠脉循环中儿茶胺流出的影响（突触前效应）。在静脉环实验中，10(-6)至10(-4)M的塞利洛尔以浓度相关的方式使对BHT 920的浓度-反应曲线发生位移，但在浓度低于10(-4)M时对甲氧明的反应无影响。在持续刺激右侧星状神经节期间，静脉注射1-10mg/kg的塞利洛尔可增加冠状窦中的儿茶胺浓度，同时降低心率。相比之下，普萘洛尔不影响儿茶胺浓度，但降低心率；萝芙辛增加儿茶胺浓度和心率；可乐定降低儿茶胺浓度和心率。这些结果与以下假设一致，即塞利洛尔除具有β1阻断活性外，还具有较弱的α2拮抗特性。
