Literature DB >> 23581180

[Hypoxic pulmonary hypertension and novel ATP-sensitive potassium channel opener: the new hope on the horizon].

Yu Jin1, Wei-Ping Xie, Hong Wang.   

Abstract

Hypoxic pulmonary hypertension (HPH) is a syndrome characterized by the increase of pulmonary vascular tone and the structural remodeling of peripheral pulmonary arteries. The aim of specific therapies for hypoxic pulmonary hypertension is to reduce pulmonary vascular resistance, reverse pulmonary vascular remodeling, and thereby improving right ventricular function. Iptakalim, a lipophilic para-amino compound with a low molecular weight, has been demonstrated to be a new selective ATP-sensitive potassium (K(ATP)) channel opener via pharmacological, electrophysiological, biochemical studies, and receptor binding tests. In hypoxia-induced animal models, iptakalim decreases the elevated mean pressure in pulmonary arteries, and attenuates remodeling in the right ventricle, pulmonary arteries and airways. Furthermore, iptakalim has selective antihypertensive effects, selective vasorelaxation effects on smaller arteries, and protective effects on endothelial cells, but no effects on the central nervous, respiratory, digestive or endocrine systems at therapeutic dose. Our previous studies demonstrated that iptakalim inhibited the effects of endothelin-1, reduced the intracellular calcium concentration and inhibited the proliferation of pulmonary artery smooth muscle cells. Since iptakalim has been shown safe and effective in both experimental animal models and phase I clinical trials, it can be a potential candidate of HPH in the future.

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Year:  2012        PMID: 23581180

Source DB:  PubMed          Journal:  Zhongguo Ying Yong Sheng Li Xue Za Zhi        ISSN: 1000-6834


  1 in total

1.  MitoKATP regulating HIF/miR210/ISCU signaling axis and formation of a positive feedback loop in chronic hypoxia-induced PAH rat model.

Authors:  Yang Lu; Jing Huang; Shuang Geng; Hao Chen; Cheng Song; Shan Zhu; Su Zhao; Mingli Yuan; Xueying Li; Hongling Hu
Journal:  Exp Ther Med       Date:  2017-02-23       Impact factor: 2.447

  1 in total

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