Publications by authors named "M D Mashkovskii"

The paper presents experimental and clinical findings of the new antiarrhythmic drug nibentan. The agent was found to be a class-III antiarrhythmic agent in terms of its electrophysiological effects and an inhibitor of the delayed rectifier potassium current in terms of its effects on the ionic channels of cardiomyocytes. The clinical trial of nibentan shows that the drug is highly effective (in 70-100% of cases) in patients with atrial flutter and fibrillation and in those with supraventricular tachycardia and it is less effective in suppressing ventricular premature contractions and tachycardia.

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Results of search for new beta-adrenoreceptor blocking agents of different effects are summarized. Derivatives of 4-hydroxyindolyl-3-acetic acid are characterized by a prolonged beta-adrenoblocking effect, cardioselective beta-adrenoblockers were found among derivatives of N,N-bis(2-hydroxy-3-phenoxypropanol)amine, and highly effective "hybrid" beta-,a-adrenoblockers were detected among derivatives of 3(5)-phenoxymethylisoxazolines and 5-phenoxymethyl-1,2,4,-oxadiasoles. Clinical studies of one of the most promising compounds of the latter series named proxodolol showed it to be a highly effective antihypertensive, antianginal, and antiglaucoma drug.

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Tetrindol, a selective inhibitor of MAOA (predominantly of serotonin oxidase) and fluoxetine, an inhibitor of serotonin neuronal uptake, were studied in psychotropic tests on mice and rats. Both drugs significantly intensified 5-hydroxytriptophan-induced head twitching, reduced the effect of reserpine and the destructive action of maximal electroshock and the scopalamine-induced transient disruption of memory in a test for conditioned response of passive avoidance in rats and mice. In a behavioral swimming test the drugs were less active.

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