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Plasma levels and excretion of two beta-adrenoceptor blocking drugs 3H-exaprolol and 3H-propranolol were observed up to 96 h after a single i.v. administration to rats. Terminal half-lives of 26.8 +/- 9.1 h and 51.3 +/- 7.5 h were found for exaprolol and propranolol, respectively. The recovery of 3H radioactivity in feces following i.v. administration of(More)
The study was designed to characterise the influence of a novel acyl-CoA:cholesterol acyltransferase inhibitor, VULM 1457, on the severity of myocardial ischaemia-reperfusion injury in a model of diabetes mellitus and hypercholesterolaemia induced by co-administration of streptozotocin and a high fat-cholesterol diet. We used Langendorff-perfused rat hearts(More)
Pharmacokinetics of cis-(-)-2,3,4,4a,5,9b-hexahydro-2,8-dimethyl- 1H-pyrido-[4,3-b]indole dihydrochloride (Stobadin; in the following briefly called STB), a pharmacologically active stereoisomer of the gamma-carboline carbidine, was studied using a 3H-labelled product. Determination of STB in biological material was based on liquid-liquid extraction from(More)
The time dependence of the distribution of intravenously injected radiolabelled Candida albicans in the body of mice was studied. The Candida cells were labelled by cultivating them 7 days at 28 degrees C in a medium containing one of the following radionuclides: 46Sc, 95Nb, 59Fe, 144ce, 89Sr, 60Co, 65Zn, 54Mn, 45Ca, 51Cr and 91Y, which are listed in(More)
The distribution of [3H]-stobadine, a pyridoindole antioxidant, was investigated in New Zealand white rabbits and their fetuses on days 20 and 27 of gestation. The concentrations of [3H]-stobadine were determined in maternal and fetal organs after oral administration in a single dose of 5.0 mg/kg. The results of the study showed that during the late period(More)
The status of nitric oxide (NO) in spontaneously hypertensive rats (SHR) is unclear and its bioavailability may be affected by imbalance with reactive oxygen species. We studied cardiovascular effects of an NO donor, pentaerythrityl tetranitrate (PETN) in SHR. We used Wistar rats, SHR and SHR treated with PETN (200 mg/kg/day). After six weeks, myocardium(More)
Stobadine, a pyridoindole antioxidant, was investigated for its placental transfer and distribution in New Zealand white rabbits on the 27th day of gestation. The concentrations of stobadine were determined in maternal and foetal organs (plasma, brain, heart) at 30, 60, 120, and 360 minutes after oral administration of the drug in a dose of 5 mg/kg. The(More)
This study examined the effects of simvastatin (10 mg/ kg) and VULM 1457 (50 mg/kg), an ACAT inhibitor, in the heart model of 6 min ischemia followed by 10 min reperfusion injury in the diabetic-hypercholesterolaemic (DM-HCH) rats. In the DM-HCH rats, the incidence of ventricular tachycardia (VT) had a tendency to be increased, while ventricular(More)
The pharmacokinetics of two beta adrenoceptor blocking drugs, exaprolol and propranolol, in rats with interrupted enterohepatic circulation was studied. The tritium-labelled drugs were given intravenously to four groups of rats: control, bile-duct cannulated, bile-duct ligated, and pretreated with neomycin. Plasma levels and excretion were observed up to 96(More)
We studied the effects of long-term administration of molsidomine and pentaerythrityl tetranitrate (PETN) on the cardiovascular system of spontaneously hypertensive rats (SHR). One control and three experimental groups of 10-week-old animals were used: 1) control Wistar rats, 2) SHR, 3) SHR treated with molsidomine in tap water (100 mg/kg/day, by gavage),(More)