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Biomedical subjects

M Matera

Publications and source records attributed to M Matera.

At least 19 recordsLinked to original sources

Effect of acetyl-L-carnitine on ethanol consumption and alcohol abstinence syndrome in rats.

The effect of acetyl-L-carnitine on alcohol consumption and its possible ability to alleviate all symptomatology of ethanol withdrawal syndrome has been investigated in rats. Alcohol-dependence was induced in animals (9-15 g/kg ethanol solution at 20% for a period of 4 days) in order to measure the effects of acetyl-L-carnitine on ethanol abstinence syndrome. The ethanol dependence phase was characterized by the onset of signs and responses of progressive severity: hyperactivity, tremors, spastic rigidity and spontaneous convulsive seizures. After 4 days, 8 h after the last ethanol administration, two groups of animals received acetyl-L-carnitine (125 mg/kg and 250 mg/kg intraperitoneally, respectively) and the intensity of the withdrawal syndrome was assessed on the basis of the appearance of tremors. The effect of acetyl-L-carnitine on voluntary alcohol consumption was investigated in a rat line selected for innate ethanol preference. For 15 days the animals could freely choose both water and/or a hydroalcoholic solution (10% p:v). Acetyl-L-carnitine was given intraperitoneally at a dose of 200 mg/kg twice daily. The water and the hydroalcoholic solution levels were checked at the same time daily. Acetyl-L-carnitine treatment significantly reduced the onset of tremors in ethanol withdrawal syndrome as well as the level of ethanol intake in alcohol-preferring rats. These results suggest a possible pharmacological role of acetyl-L-carnitine in the treatment of alcohol dependence.

Acetylcarnitine↗

Effects of pivagabine on psychophysical performance and behavioural response in experimental models of stress.

The effect of pivagabine (4-[(2,2-dimethyl-1-oxopropyl)amino]butanoic acid, CAS 69542-93-4, Tonerg), a synthetic molecule with neuromodulatory activity, was evaluated on a series of behavioural parameters in rats exposed to various stimuli, with the aim of evaluating the response to stress (open field exploration, water maze, psychic conflict), conditioning (active and passive avoidance and avoidance retention, aggressiveness, extinction of conditioned responses), learning and performing of specific psychophysical tests (rota-rod, ballasted swimming, taut thread). Pivagabine induced significant improvement of stress-related tests by reducing the anxiety-producing reactions related to the various experimental settings. In conditioning tests an improvement in learning of conditioned responses was observed at lower dosages (10 and 50 mg/kg); an opposite effect was obtained with higher dosages (100 and 200 mg/kg). Pivagabine did not influence the retention nor the extinction of conditioned responses. Pivagabine induced a marked improvement of all motor performance tests in young and in aged animals. By contrast with benzodiazepines, pivagabine did not alter the ability of learning tasks, the motor performance and the aggressive behaviours. It is likely that the observed effects of pivagabine are mediated by inhibition of release of corticotropin-releasing factor, a neurohormone involved in stress-generating mechanisms.

Animals↗

Pharmacokinetic study of the relative bioavailability and bioequivalence after oral intensive or repeated short term treatment with two polyamino acid formulations.

The authors studied the relative bioequivalence and bioavailability of two oral polyamino-acid formulations (packet and flacon), based on 4 amino acids (L-glutamine, L-phosphoserine, L-phosphothreonine and L-arginine) in association with vitamin B12 (Bio-logos, Sigma Tau Pharma S.A). Open-trial testing was carried out after intensive treatment and on the attainment of sustained levels. 50 healthy volunteers (27 males, 23 females), ranging in age from 23 to 32 years, were included in the study. The pharmacokinetic behaviour of the various active ingredients was examined at a haematic level. Possible undesirable side-effects, resulting from treatment, were also examined during the study. The mean pharmacokinetic constants considered (Ke1, Cmax and t1/2) generated an almost overlapping AUC (area under the curves) for all homologous components contained in both pharmaceutical forms. This indicates almost complete bioequivalence. The mean index for the rate of relative bioavailability was, in fact, estimated to be 106.3 +/- 12.4%. Repeated treatment did not appear to disturb the absorption mechanisms of the active ingredients contained in either of the two formulations examined, maintaining the relative bioavailability relationship within a negligible range, with a statistically non-significant difference (Student's t test for coupled data). A few episodes, characterized by slight increases in excitability, were reported for both preparations in two patients (4%).

Administration, Oral↗

MAOI activity of some novel series of substituted thiazol-2-yl-hydrazines.

Three series of 2-thiazolylhydrazines were synthetized and evaluated for their MAO inhibitory (MAOI) activity, both by in vivo tests, to assay their influence on several MAOI activity-related parameters (the variation on blood pressure induced by tyramine and clonidine and L-amfetamine-induced hypermotility) and in vitro tests, to assay their effect on rat brain mitochondria by a kinuramine fluorimetric assay. In vivo, all the tested compounds significatively influenced the evaluative parameters used. As regards in vitro test, all compounds displayed MAOI activity at a concentration of 1.10(-4) mol.l-1, which was significant in several cases. In the discussion of the results, the influence of the structure on the biological activity of the prepared compounds was delineated.

Amphetamine↗

Anticoagulant activity of galactosaminoglucuronoglycan: a pharmacological study.

An investigation was carried out to evaluate possible interference by mucopolysaccharide galactosaminoglucuronoglycans on blood clotting processes. Results obtained have demonstrated, both in vivo and in vitro, that the biopolymer has no influence on the principal blood clotting parameters taken into consideration, as regards both a single administration and treatments repeated for 30 days.

Animals↗

Synthesis and evaluation of the analgesic and antiinflammatory activities of N,N'-bis(2-hydroxybenzoyl)-diaminoalkanes.

The analgesic and antiinflammatory activities of some N,N'-bis(2-hydroxybenzoyl)-diaminoalkanes 3 a-l were studied. The compounds were prepared very conveniently by fusion of phenyl salicylate 2 and diaminoalkanes 1 a-l. The pharmacological activities were influenced by the number of carbon atoms in the polimethylenic chain. Some derivatives were more effective and less gastrolesive than salicylamide.

Analgesics↗

Researches on antiinflammatory agents. Studies on some new 3-(pyrazol-5-yl)-1,2,3-benzotriazin-4(3H)-ones and -quinazolin-4(3H)-ones.

Following our research on analgesic and antiinflammatory active compounds containing the pyrazole nucleus, a number of 3-(pyrazol-5-yl)-1,2,3-benzotriazin-4(3H)-ones and quinazolin-4(3H)-ones was synthetized and tested. The results of tests for analgesic, antiexudative and antioedema activities, as well as for induction of lesion in the gastric mucosa, are reported and discussed.

Animals↗