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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TREATMENT OF CARDIOVASCULAR DISEASE IN CHRONIC AND END STAGE KIDNEY DISEASE
Cardiovascular disease still remains the leading cause of death in Chronic and End Stage Kidney Disease, accounting for more than half of all deaths in dialysis patients. During the past decade, research has been focused on novel therapeutic agents that might delay or even reverse cardiovascular disease and vascular calcification, ...read more
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