Maloteaux J M, Haiech J, De Campeneere D, Berta P, Vidal N
Arzneimittelforschung. 1986 Aug;36(8):1194-8.
In experimental and clinical investigations, 2-(diethylamino)ethyl-tetrahydro-alpha-(1-naphthyl-methyl)-2-furanpro pionate (naftidrofuryl, Praxilene) appears to improve blood flow and microcirculation in ischemic areas. In order to define the mechanism by which the drug may exert its vascular effects, the binding affinity of naftidrofuryl toward various receptors was studied. From this biochemical study, it appeared that, in therapeutic doses, naftidrofuryl selectively inhibited the binding of spiperone or ketanserin to serotonin S2 receptors. This finding was corroborated in physiological models such as isolated rat caudal arteries or preparations of aortic myocytes. Naftidrofuryl effectively blocked the constrictive effect of serotonin on the artery in a dose-dependent, competitive manner. It also strongly inhibited the formation of serotonin-stimulated inositol triphosphate in the myocytes. From these good correlations between biochemical and physiological data it is concluded that the beneficial effects of naftidrofuryl on ischemic tissue perfusion may be partly explained on the basis of selective antiserotonergic S2 properties.
在实验和临床研究中，2 - （二乙氨基）乙基 - 四氢 - α - （1 - 萘基甲基） - 2 - 呋喃丙酸酯（萘呋胺酯，脑心舒）似乎能改善缺血区域的血流和微循环。为了确定该药物发挥血管作用的机制，研究了萘呋胺酯对各种受体的结合亲和力。从这项生化研究来看，在治疗剂量下，萘呋胺酯能选择性抑制螺哌隆或酮色林与5 - 羟色胺S2受体的结合。这一发现在诸如离体大鼠尾动脉或主动脉肌细胞制剂等生理模型中得到了证实。萘呋胺酯以剂量依赖性、竞争性方式有效阻断5 - 羟色胺对动脉的收缩作用。它还强烈抑制肌细胞中5 - 羟色胺刺激的肌醇三磷酸的形成。基于生化和生理数据之间的这些良好相关性，可以得出结论，萘呋胺酯对缺血组织灌注的有益作用部分可基于选择性抗5 - 羟色胺能S2特性来解释。
