Polish journal of pharmacology and pharmacy最新文献

The effect of chronic electroconvulsive seizure on the blood brain barrier permeability to albumin was investigated in the male rats. Evans blue was used as a blood brain barrier tracer. The following situations were studied: Acute electroshock: a. one electroshock stimulus, b. ten electroshock stimuli. Chronic electroshock: a) group of animals were pretreated with electroshock given as one electroshock (ES) every other day (ES x 7); b) chronic electroshock + one electroshock, c) chronic electroshock + ten repeated electroshocks. As a result, chronic electroshock per se does not effect the blood-brain barrier permeability.

Captopril, an angiotensin converting enzyme inhibitor, was evaluated for a potential antidepressive activity in several animal models. The drug administered in doses of 3-30 mg/kg ip neither affected the reserpine- or apomorphine-induced hypothermia in mice nor reduced the immobility time in the forces swimming test in mice and rats. Moreover, captopril administered repeatedly (10 mg/kg ip, twice daily for 14 days) neither changed the density or affinity of cortical beta-adrenoceptors nor modified the nomifensine-induced locomotor hyperactivity in rats. These results suggest that captopril has no antidepressant-like activity in animal models.

Several new alpha-aminoderivatives of gamma-(p-chlorophenyl)-tetrahydrofuran-2-one were synthesized. alpha-Aminoderivatives of beta-(p-chlorobenzoyl)-propionic acid 2-13 were used as the substrates. After the reduction with NaBH4 at 10-12 degrees C and cyclization the compounds were converted into the appropriate derivatives of tetrahydrofuran-2-one 16-26. In pharmacological tests compounds 9 and 26 abolished the aggressiveness in isolated mice while compound 8 showed antiinflammatory activity.

Effects of single and repeated administration of the MAO-A-inhibitor moclobemide (MOC) on the spontaneous locomotor activity and the locomotor hyper- and hypoactivity induced by d-amphetamine and clonidine, resp., in male Wistar rats were studied in both the light (L) and the dark (D) phase of the diurnal cycle (L:0700-1900 h). In the light phase, two hours after single administration, MOC (10 and 50 mg/kg po) increased the basal activity and a dose of 50 mg/kg decreased the exploratory and gross activities and enhanced the effects of amphetamine and clonidine. On the other hand, in the dark phase MOC (50 mg/kg) increased the gross activity and potentiated amphetamine hyperactivity. Only exploration was diminished to the same extent as in the light phase. After repeated administration MOC increased only the gross activity in the light phase. In the dark phase, however, MOC diminished exploration and potentiated the d-amphetamine hyperactivity. MOC, in both doses used, diminished food and water consumption and the body weight gain during the treatment period. These results demonstrate that MOC influences the behavior of rats in a phase-dependent manner after both single and repeated administration.

Pharmacokinetic parameters of thiamazole were compared in two groups of patients with hyperthyroidism due to Graves-Basedow disease, differing in the period required to achieve clinical euthyrosis (less than 28 days, group R, n = 23, and not less than 35 days, group D, n = 18) after treatment with the "full" dose of the drug. The drug absorption from the GI tract in both groups was similar, but the serum concentrations of the drug (Cmax and AUC) were higher, and distribution volume and total clearance lower in the R than in D group. No evidence was found for the importance of initial plasma levels of thyroxine or triiodothyronine on pharmacokinetic parameters of thiamazole.