Ryckewaert J J, Maurel A, Marguerie G
Unité INSERM 217, DRF/LBIO/Laboratoire d'Hématologie, Grenoble, France.
Haemostasis. 1990;20(3):181-91. doi: 10.1159/000216125.
The effect of buflomedil (Fonzylane; Laboratoire Lafon, Maisons-Alfort, France) on platelet function, a drug used clinically for the treatment of peripheral vascular diseases, was investigated in vitro. The compound significantly inhibits epinephrine-induced aggregation at the micromolar level. At higher doses (approximately 1 mM), a weak inhibition of ADP- and collagen-induced aggregation was observed; at these concentrations, buflomedil inhibits granular secretion and the interaction of fibrinogen with its receptor on platelet. Further investigations indicate that the drug affects calcium uptake at the membrane level and inhibits the binding of [3H]-yohimbine to the same extent as observed with phentolamine. The IC50 determined from competition binding assays was 1 +/- 0.5 microM. This value was consistent with the affinity constant approximated for the binding of [3H]-buflomedil to non-stimulated platelets. Taken-together, these results indicate that the vasoactive compound buflomedil is a weak antiaggregating agent which exhibits alpha 2-adrenergic antagonistic properties.
在体外研究了临床上用于治疗外周血管疾病的药物丁咯地尔（Fonzylane；法国迈松阿尔福拉丰实验室）对血小板功能的影响。该化合物在微摩尔水平上显著抑制肾上腺素诱导的聚集。在较高剂量（约1 mM）时，观察到对ADP和胶原诱导的聚集有微弱抑制作用；在这些浓度下，丁咯地尔抑制颗粒分泌以及纤维蛋白原与其在血小板上的受体的相互作用。进一步研究表明，该药物在膜水平影响钙摄取，并与酚妥拉明一样程度地抑制[3H] -育亨宾的结合。从竞争结合试验确定的IC50为1±0.5 microM。该值与[3H] -丁咯地尔与未刺激血小板结合的近似亲和常数一致。综上所述，这些结果表明血管活性化合物丁咯地尔是一种具有α2 -肾上腺素能拮抗特性的弱抗聚集剂。
