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ISSN 2522-9028 (Print)
ISSN 2522-9036 (Online)
DOI: https://doi.org/10.15407/fz

Fiziologichnyi Zhurnal

is a scientific journal issued by the

Bogomoletz Institute of Physiology
National Academy of Sciences of Ukraine

Editor-in-chief: V.F. Sagach

The journal was founded in 1955 as
1955 – 1977 "Fiziolohichnyi zhurnal" (ISSN 0015 – 3311)
1978 – 1993 "Fiziologicheskii zhurnal" (ISSN 0201 – 8489)
1994 – 2016 "Fiziolohichnyi zhurnal" (ISSN 0201 – 8489)
2017 – "Fiziolohichnyi zhurnal" (ISSN 2522-9028)

Fiziol. Zh. 2010; 56(4): 59-65


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

Strutyns'kyĭ RB

    O.O. Bogomoletz Institute of Physiology, National Academy of Science of Ukraine, Kyiv, Ukraine
DOI: https://doi.org/10.15407/fz56.04.059

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: KATP channels, vasodilatation, arterial blood pressure, floñalin.

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