title: [Effect of a new activator of adenosine triphosphate-sensitive potassium channels flocalin on the glucose level in blood].
abstract: In experiments on the anaesthetized dogs we investigated the influence of a new fluorine-containing opener of ATP-sensitive potassium channels of sarcolemal and mitochondrial membranes flocalin on the level of glucose in arterial blood at physiological conditions and under ischemia (90 min) and reperfusion (180 min) of myocardium. It was shown that intravenous introduction of flocalin in doses 0,1 - 1,0 mg/kg did not change the level of glucose in blood. In experiments with ischemia-reperfusion of myocardium, flocalin also did not increase the level of glucose during all experiment (5,5 hours) after intragastric (with a help of catheter) introduction of drug form (tablets) at cardiorotective dose of 2,2 mg/kg. However, intravenous introduction of flocalin in the dose of 1,5 mg/kg, which 15 times exceeded a cardioprotective dose of 0,1 mg/kg increased the glucose level 1,33 fold. It should be noted that this increase was not sustained and the level of glucose restored to the initial level within 1 hour. Identical changes of indexes of cardiohemodynamic and the level of glucose in arterial blood under introduction of identical doses of flocalin at the beginning and at the end of experiment (total dose of flocalin reached 4 - 4,5 mg/kg) can testify the absence of cumulative effect of flocalin at these experimental conditions. Thus, strong cardioprotective properties, hypotoxicity and the absence of meaningful changes in a carbohydrate exchange allow to consider a new fluorine-containing opener of K(ATP) channels of flocalin as perspective drug for clinical use.
authors.forename: R B
authors.initials: RB
authors.lastname: Strutyns'kyĭ
authors.forename: R A
authors.initials: RA
authors.lastname: Rovenets'
authors.forename: O P
authors.initials: OP
authors.lastname: Neshcheret
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001786:Blood Glucose / Q000378:metabolism*; D002316:Cardiotonic Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D004285:Dogs; D004305:Dose-Response Relationship, Drug; D005260:Female; D007275:Injections, Intravenous; D054086:KATP Channels / Q000819:agonists*; D008297:Male; D015428:Myocardial Reperfusion Injury / Q000097:blood / Q000378:metabolism / Q000517:prevention & control*; D020110:Pinacidil / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use; D013997:Time Factors
chemical_list: D001786:Blood Glucose; D002316:Cardiotonic Agents; D054086:KATP Channels; C559719:N-(4-difluoromethoxyphenyl)-N'-pinacolyl-N''-cyanoguanidine; D020110:Pinacidil