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[硝苯苄胺啶(福立多)的生化效应——一种新型钙拮抗剂及1,4 - 二氢吡啶衍生物]

[Biochemical effects of ryodipine (foridon)--a new calcium antagonist and derivative of 1,4-dihydopyridine].

作者信息

Simkhovich B Z, Mezhapuke R Ia, Dubur G Ia

出版信息

Farmakol Toksikol. 1988 May-Jun;51(3):30-4.

PMID:2842181
Abstract

Ryodipine (foridon)--2, 6-dimethyl-3,5-dicarbomethoxy-4-(o-difluoromethoxyphenyl)-1, 4-dihydropyridine--similarly to nifedipine but at a lesser degree than nicardipine causes an increase of cAMP concentration in the slices of the rabbit myocardium and aorta. This property of 1,4-dihydropyridines is reflected in their effect on the uptake of 45Ca2+ by the myocardial strips. In the range of concentrations of 10(-4)-10(-6)M inhibition of 45Ca2+ transport is enhanced with a decrease of concentrations of the drugs. Under inactivation of potential-dependent transport of Ca2+, 1,4-dihydropyridines enhance the uptake of 45Ca2+. The similar effect was found at incubation of the myocardial slices in a polarizing buffer (2.68 mM K+). Verapamil, irrespective of the degree of depolarization (60,123 mM K+), suppressed in a linear dependence the uptake of 45Ca2+ and failed to influence this process in the absence of potential-dependent transport of Ca2+. By its biochemical effects ryodipine does not differ from the known derivatives of 1,4-dihydropyridine but has, like nifedipine and nicardipine, significant differences as compared with verapamil.

摘要

利奥地平(福洛地平)——2,6 - 二甲基 - 3,5 - 二羧酸甲氧基 - 4 - (邻 - 二氟甲氧基苯基)-1,4 - 二氢吡啶——与硝苯地平类似,但程度小于尼卡地平,可使兔心肌和主动脉切片中的环磷酸腺苷(cAMP)浓度升高。1,4 - 二氢吡啶的这一特性反映在它们对心肌条带摄取45Ca2+的影响上。在10^(-4) - 10^(-6)M的浓度范围内,随着药物浓度的降低,45Ca2+转运的抑制作用增强。在钙的电位依赖性转运失活的情况下,1,4 - 二氢吡啶可增强45Ca2+的摄取。在极化缓冲液(2.68 mM K+)中孵育心肌切片时也发现了类似的效果。维拉帕米,无论去极化程度如何(60、123 mM K+),均呈线性抑制45Ca2+的摄取,并且在没有钙的电位依赖性转运时对该过程没有影响。就其生化作用而言,利奥地平与已知的1,4 - 二氢吡啶衍生物没有差异,但与维拉帕米相比,它与硝苯地平和尼卡地平一样,存在显著差异。

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