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新型钙通道拮抗剂凡托法隆对动脉粥样硬化兔模型中血管成形术诱导的血管痉挛的作用。

Effect of fantofarone, a new Ca2+ channel antagonist, on angioplasty-induced vasospasm in an atherosclerotic rabbit model.

作者信息

Dongay B, Dol-Gleizes F, Herbert J M

机构信息

Haemobiology Research Department, Sanofi Recherche, Toulouse, France.

出版信息

Biochem Pharmacol. 1998 Jun 15;55(12):2047-50. doi: 10.1016/s0006-2952(98)00026-4.

Abstract

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.

摘要

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。

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