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Fiziolohichnyĭ zhurnal
Article . 2010 . Peer-reviewed
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The vasodilation effects of flokalin, a fluorine-containing K(ATP) channel opener

Вазодилататорні ефекти флокаліну фторвмісного активатора аденозинтрифосфатчутливих калієвих каналів
Authors: R B, Strutyns'kyĭ;

The vasodilation effects of flokalin, a fluorine-containing K(ATP) channel opener

Abstract

In experiments on anesthetized dogs it was shown that the amplitude and duration of hypotensive effect of flocalin, a fluorine-containing pinacidil analogue, were dose-dependent and similar to those evoked by the known ATP-sensitive potassium channel opener pinacidil. However, flocalin appeared to be 3.5 times less toxic than pinacidil. Registration of systemic arterial pressure (SAP) has shown that following intravenous introduction of the threshold dose of flocalin (0.05 mg/ kg) the dilatation lasts around three minutes with the amplitude 9.52% +/- 2.01% (n=7, P < 0.05). Introduction of flocalin in a dose 0.5 mg/kg and above reduced SAP on more than 37%. Flocalin at 0.5, 0.75, 1.0 and 1.5 mg/kg reduced SAP by 42.07 +/- 6.18 (n=5, P < 0.05); 44.22 +/- 4.87 (n=3, P < 0.05); 44.3 +/- 4.59 (n=5, P < 0.05) and 66.28 +/- 3.15 mm Hg (n=3, P < 0.05), accordingly. Intravenous introduction of high doses of flocalin (0.75-1.5 mg/kgs) quite often reduced SAP to 40-50 mm Hg. However, such dangerous reduction in arterial pressure was comparatively short and lasted not more than 15 minutes, and then (usually within an hour) SAP gradually restored. Introduction of flocalin in hip artery, while measuring the perfusion pressure, produced practically similar results. In our opinion, the optimal cardioprotective doses of flocalin were 0.1 and 0.2 mg/kg. In experiments with acute ischemia and reperfusion of myocardium, preischemic introduction of flocalin at 0.1 and 0.2 mg/kg reduced an infarct size of myocardium by 37-40% and reduced SAP within first 5 and 25 minutes, accordingly.

Keywords

Male, Time Factors, Dose-Response Relationship, Drug, Pinacidil, Vasodilator Agents, Blood Pressure, Fluorine, Vasodilation, Dogs, Injections, Intra-Arterial, KATP Channels, Injections, Intravenous, Animals, Female, Ion Channel Gating

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citations
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
8
Average
Average
Average
gold