Synthesis of some hydroxynaphthazarins and their cardioprotective effects under ischemia-reperfusion in vivo.

A series of hydroxynaphthazarins has been synthesized. Some of them were found in in vivo experiments to be protectors of myocardium under ischemia-reperfusion and to reduce the infarction zone by 50% without any adverse effect. All compounds exhibit a moderate or small toxicity and are active in low doses.

Misoprostol and dalargin for the inpatient treatment of duodenal ulcer in the USSR.

In the USSR, uncomplicated duodenal ulcer is usually managed in an inpatient setting. A double-blind, randomized, double-dummy, multiclinic, comparative trial examined the safety and efficacy of oral misoprostol (200 micrograms qid) and intramuscular dalargin (1 mg bid) in duodenal ulcer healing. Dalargin, an enkephalin peptide with gastric antisecretory and cytoprotective properties, is commonly used in the USSR for treating peptic ulcer.

Reduction of ventricular arrhythmias by phosphocreatine (Neoton) in patients with acute myocardial infarction.

On the basis of the positive results of recent experimental research, a clinical trial of phosphocreatine (Neoton) was carried out in 60 randomized patients with acute myocardial infarction (30 patients in the Neoton group and 30 patients in the control group). Neoton was given intravenously not later than 6 hours after the onset of symptoms, in a dose of 2 gm as a bolus injection, followed by a 2-hour infusion at the rate of 4 gm/hr. Holter monitoring for 24 hours showed a significant decrease in the frequency of ventricular premature beats: in the Neoton-treated group the total number of ventricular premature beats for 24 hours was 690 +/- 179 vs 2468 +/- 737 in the control group (p less than 0.

Protection of ischemic myocardium by exogenous phosphocreatine (neoton): pharmacokinetics of phosphocreatine, reduction of infarct size, stabilization of sarcolemma of ischemic cardiomyocytes, and antithrombotic action.

The effect of exogenous phosphocreatine on ischemic myocardium was studied in experimental infarction in rabbits and in total ischemia of pig heart tissue (in vitro). It is shown that single dose administration of phosphocreatine is followed by its rapid clearance from blood plasma (with a half lifetime of 4-6 min), but constantly high plasma concentration of phosphocreatine can be maintained by its intravenous infusion. When administered by this method into rabbits during experimental myocardial infarction, phosphocreatine reduces by 40% the size of the necrotic zone.