Effects of dihydropyridine calcium channel modulators in the heart: pharmacological and radioligand binding correlations.

Effects of dihydropyridine calcium channel modulators in the heart: pharmacological and radioligand binding correlations.
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二氢吡啶钙通道调节剂对心脏的影响:药理学和放射性配体结合相关性。

DOI:
10.1016/s0006-291x(84)80380-0
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发表时间:
1984
影响因子:
3.1
通讯作者:
Vaghy,PL
Vaghy,PL
中科院分区:
生物学4区
文献类型:
--
作者:
Schwartz,A;Grupp,IL;Grupp,G;Williams,JS;Vaghy,PL

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在离体和完整的心脏标本中,Bay k8644产生浓度依赖性正性肌力作用,随后产生负性肌力作用。尼莫地平在低浓度时产生轻微的正性肌力作用,在高浓度时产生通常的负性肌力作用。放射性配体结合实验表明,平衡解离常数,与药理学数据一起,表明二氢吡啶类结合受体亚型,并具有不同的内在活动。
Bay k 8644 produced a concentration-dependent positive inotropic effect followed by a negative inotropic effect in isolated and intact cardiac preparations. Nimodipine in low concentrations produced slight positive inotropy and in higher concentrations, the usual negative inotropic action. Radioligand binding experiments revealed equilibrium dissociation constants that, taken together with the pharmacological data, suggest that dihydropyridines bind to receptor subtypes and have varying intrinsic activities.