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V Klimek

Publications and source records attributed to V Klimek.

60 records · Page 4Linked to original sources

Central effects of repeated treatment with bupropion.

The effect of bupropion, a new clinically active antidepressant drug, administered repeatedly to rats and mice, was compared with that of imipramine. The drugs were given orally twice a day for 14 days, bupropion in a dose of 20 mg/kg, imipramine--10 mg/kg. The action of bupropion was studied in the following tests: clonidine-induced aggression in mice, open field in rats, amphetamine-induced hypermotility in rats, clenbuterol-induced hyperthermia in rats kept at high ambient temperature. Moreover, the effect of bupropion on 3H-prazosin binding to membranes from the cerebral cortex was measured. On the basis of the results obtained it may be concluded that in some tests chronically administered bupropion acts like imipramine; as both drugs potentiate the amphetamine-enhanced locomotor activity, attenuate the hyperthermic response to clenbuterol and increase the number of 3H-prazosin binding sites in the cerebral cortex.

Aggression↗

Central effects of repeated treatment with CGP 37849, a competitive NMDA receptor antagonist with potential antidepressant activity.

CGP 37849, a competitive NMDA receptor antagonist, was administered repeatedly (10 mg/kg po, twice daily for 14 days) to male Wistar rats. In behavioral studies it did not affect the locomotor activity, but enhanced the d-amphetamine-induced hyperactivity. Biochemical studies of the concentrations of dopamine (DA), 3,4-dihydroxyphenylacetic acid (DOPAC), homovanillic acid (HVA), noradrenaline (NA), 5-hydroxytryptamine (5-HT) and 5-hydroxyindole acetic acid (5-HIAA) in the rat cerebral cortex, striatum and nucleus accumbens showed that only the concentrations of DOPAC (an increase) and NA (a decrease) were changed in the nucleus accumbens. Repeated administration of CGP 37849 increased the density of dopamine D1 receptors labelled with [3H]-SCH 23390 in the rat striatum, but not in the limbic forebrain, having exerted no effect on the density of D2 receptors labelled with [3H]-spiperone. The density of alpha 1- and beta-adrenoceptors, labelled with [3H]-prazosin and [3H]-dihydroalprenolol, respectively, were unchanged in the cerebral cortex. The obtained results indicate that in some experimental paradigms CGP 37849 given repeatedly produces effects similar to those of typical antidepressant drugs.

2-Amino-5-phosphonovalerate↗

The effect of MK-801 and imipramine on beta-adrenergic and 5-HT2 receptors in the chronic mild stress model of depression in rats.

Chronic exposure (8 weeks) to sequential application of mild stressors caused the increase in the density (Bmax) of beta-adrenergic and 5-HT2 receptors in the rat cerebral cortex. MK-801 given chronically (5 weeks) decreased beta-adrenergic receptors density in both control and stressed rats, whereas it decreased the density of 5-HT2 receptors in control rats only. On the other hand, imipramine administered for 5 weeks reduced the number of beta-adrenergic and 5-HT2 receptors in both control and stressed rats.

Animals↗

Rapid down-regulation of beta-adrenergic receptors evoked by combined forced swimming test and CGP 37849--a competitive antagonist of NMDA receptors.

The influence of CGP 37849, a competitive antagonist of NMDA, receptors and desipramine (DMI) on the density of beta-adrenergic receptors in rats exposed to the forced swimming test was investigated. CGP 37849 (10 mg/kg) and DMI (15 mg/kg), given twice to rats (24 h apart), or the forced swimming test alone failed to alter the density of beta-adrenergic receptors in the rat cortex, as tested using [3H]dihydroalprenolol ([3H]DHA). However, in rats injected with CGP 37849 (10 mg/kg) or DMI (15 mg/kg) and exposed to the forced swimming test, it was found that the density of beta-adrenergic receptors in the cortex was decreased. It was also observed that CGP 37849 used in a dose which decreased the density of beta-adrenergic receptors reduced the immobility time in a manner similar to DMI. It is concluded that CGP 37849 may evoke similar adaptive receptor changes as anti-depressant drugs which-in turn-suggests antidepressant-like properties of CGP 37849.

2-Amino-5-phosphonovalerate↗