Bou J, Gras J, Cortijo J, Morcillo E J, Llenas J, Palacios J M
Almirall Prodesfarma, Research Centre, Barcelona, Spain.
Cephalalgia. 2001 Oct;21(8):804-12. doi: 10.1046/j.1468-2982.2001.218233.x.
This paper describes the vascular effects of almotriptan in comparison with sumatriptan in human vessels and tissues in vitro. The contractile properties of almotriptan and sumatriptan were evaluated in vitro in the following arteries: meningeal, temporal, basilar, internal carotid, ophthalmic, pulmonary and coronary. In addition, the effects of almotriptan on the pulmonary vein and on bronchial tissues were studied. Almotriptan showed selectivity of action for migraine-related arteries (i.e. contractile EC(50) of 30 and 700 nm for meningeal and temporal arteries, respectively), whereas the effect on arteries supplying blood to the brain was lower. The contractile effect of almotriptan was lower than that of sumatriptan in pulmonary arteries, whereas in bronchial preparations no clinically relevant contractile responses were observed for either almotriptan or sumatriptan. In ophthalmic arteries the contractile effects of almotriptan and sumatriptan were similar, whereas lower contractile effects were obtained with almotriptan than with sumatriptan in coronary arteries.
本文描述了阿莫曲坦与舒马曲坦相比,在体外人体血管和组织中的血管效应。在以下动脉中对阿莫曲坦和舒马曲坦的收缩特性进行了体外评估:脑膜动脉、颞动脉、基底动脉、颈内动脉、眼动脉、肺动脉和冠状动脉。此外,还研究了阿莫曲坦对肺静脉和支气管组织的影响。阿莫曲坦对偏头痛相关动脉表现出作用选择性(即对脑膜动脉和颞动脉的收缩EC50分别为30和700纳米),而对供应脑部血液的动脉影响较小。在肺动脉中,阿莫曲坦的收缩作用低于舒马曲坦,而在支气管制剂中,未观察到阿莫曲坦或舒马曲坦产生具有临床意义的收缩反应。在眼动脉中,阿莫曲坦和舒马曲坦的收缩作用相似,而在冠状动脉中,阿莫曲坦的收缩作用低于舒马曲坦。