Abstract
The excessive contraction of small arteries under high blood pressure is the main contributor to the pathological change of hypertension. Current anti-hypertensive drugs, which lack a selective effect on small arteries in a hypertensive state, may cause many adverse effects. We have developed a novel opener of ATP-sensitive potassium channels, iptakalim, the vasorelaxing action of which is determined by the hypertensive status of small arteries. In conscious strokeprone, spontaneously hypertensive rats and “two-kidneys, one-clip” renal hypertensive dogs, this compound produced long-lasting hypotensive effects, with no tolerance. Furthermore, it exerted a protective effect against hypertensive damage to target organs. Given its potency and fewer side effects, iptakalim hydrochloride is a promising drug for the treatment of hypertension.
Keywords: hypertension, atp-sensitive potassium channel, iptakalim, small artery, vasodilator, side effects, selective hypotensive efficacy, cardiovascular remodeling
Current Vascular Pharmacology
Title: Targeting Small Arteries of Hypertensive Status with Novel ATP-Sensitive Potassium Channel Openers
Volume: 3 Issue: 2
Author(s): Hai Wang, Ying-Li Zhang and Yu-Ping Chen
Affiliation:
Keywords: hypertension, atp-sensitive potassium channel, iptakalim, small artery, vasodilator, side effects, selective hypotensive efficacy, cardiovascular remodeling
Abstract: The excessive contraction of small arteries under high blood pressure is the main contributor to the pathological change of hypertension. Current anti-hypertensive drugs, which lack a selective effect on small arteries in a hypertensive state, may cause many adverse effects. We have developed a novel opener of ATP-sensitive potassium channels, iptakalim, the vasorelaxing action of which is determined by the hypertensive status of small arteries. In conscious strokeprone, spontaneously hypertensive rats and “two-kidneys, one-clip” renal hypertensive dogs, this compound produced long-lasting hypotensive effects, with no tolerance. Furthermore, it exerted a protective effect against hypertensive damage to target organs. Given its potency and fewer side effects, iptakalim hydrochloride is a promising drug for the treatment of hypertension.
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Cite this article as:
Wang Hai, Zhang Ying-Li and Chen Yu-Ping, Targeting Small Arteries of Hypertensive Status with Novel ATP-Sensitive Potassium Channel Openers, Current Vascular Pharmacology 2005; 3 (2) . https://dx.doi.org/10.2174/1570161053586895
DOI https://dx.doi.org/10.2174/1570161053586895 |
Print ISSN 1570-1611 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6212 |
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