Dipartimento di Chimica, Università degli Studi di Perugia, via Elce di Sotto 8, 06123 Perugia, Italia.
Curr Med Chem. 2012;19(25):4306-23. doi: 10.2174/092986712802884204.
1,4-Dihydropyridines were introduced in the last century for the treatment of coronary diseases. Then medicinal chemists decorated the 1,4-DHP nucleus, the most studied scaffold among L-type calcium channel blockers, achieving diverse activities at several receptors, channels and enzymes. We already described (Ioan et al. Curr. Med. Chem. 2011, 18, 4901-4922) the effects of 1,4-DHPs at ion channels and G-protein coupled receptors. In this paper we continue the analysis of the wide range of biological effects exerted by compounds belonging to this chemical class. In particular, focus is given to the ability of 1,4-DHPs to revert multi drug resistance that, after over 20 years of research, continues to be of great interest. We also describe activities on other targets and the action of 1,4-DHPs against several diseases. Finally, we report and review the interaction of 1,4-DHPs with the hERG channel, transporters and phase I metabolizing enzymes. This work is a starting point for further exploration of the 1,4-DHP core activities on targets, off-targets and antitargets.
1,4-二氢吡啶类在上世纪被引入用于治疗冠心病。随后,药物化学家对 1,4-DHP 核进行了修饰,这是 L 型钙通道阻滞剂中研究最多的支架,在多种受体、通道和酶上实现了多种活性。我们已经描述了(Ioan 等人,《当代医学化学》,2011 年,第 18 卷,第 4901-4922 页)1,4-DHPs 在离子通道和 G 蛋白偶联受体上的作用。在本文中,我们继续分析该化学类别的化合物所具有的广泛生物学效应。特别关注的是 1,4-DHPs 逆转多药耐药的能力,经过 20 多年的研究,这仍然是一个非常感兴趣的问题。我们还描述了其他靶点的活性以及 1,4-DHPs 对几种疾病的作用。最后,我们报告并回顾了 1,4-DHPs 与 hERG 通道、转运体和 I 相代谢酶的相互作用。这项工作为进一步探索 1,4-DHP 核心在靶点、非靶点和抗靶点上的活性提供了一个起点。