Dongay B, Dol-Gleizes F, Herbert J M
Haemobiology Research Department, Sanofi Recherche, Toulouse, France.
Biochem Pharmacol. 1998 Jun 15;55(12):2047-50. doi: 10.1016/s0006-2952(98)00026-4.
In order to prevent and treat angioplasty-induced vasospasm, we investigated the effects of a new Ca2+ channel antagonist, fantofarone, a nondihydropyridine compound with a novel site of action on the L-type Ca2+ channel, in an animal model of angioplasty in rabbits with femoral atherosclerotic lesions. Vasospasm which occurred in saline-treated animals following angioplasty was markedly reduced by fantofarone (50 microg/kg, i.v.) at both the distal and proximal sites. Although it totally inhibited distal vasospasm, isosorbide dinitrate (0.3 mg/kg, i.v.) did not significantly affect proximal diameter decrease. Verapamil (0.2 mg/kg, i.v.) was much less potent than fantofarone in reducing angioplasty-induced vasospasm. Our results confirm the preventive effects of Ca2+ blockers on this phenomenon and extend this observation to a potent compound: fantofarone.
为了预防和治疗血管成形术诱发的血管痉挛,我们在患有股动脉粥样硬化病变的兔血管成形术动物模型中,研究了一种新型钙通道拮抗剂凡托法隆(fantofarone)的作用。凡托法隆是一种非二氢吡啶类化合物,作用于L型钙通道的新位点。血管成形术后,生理盐水处理的动物发生的血管痉挛,在远端和近端部位均被凡托法隆(50微克/千克,静脉注射)显著减轻。虽然硝酸异山梨酯(0.3毫克/千克,静脉注射)完全抑制了远端血管痉挛,但对近端直径减小无明显影响。维拉帕米(0.2毫克/千克,静脉注射)在减轻血管成形术诱发的血管痉挛方面,效力远低于凡托法隆。我们的结果证实了钙通道阻滞剂对这一现象的预防作用,并将这一观察结果扩展到一种强效化合物:凡托法隆。