Because of the important glutamatergic mediation of the behavioral effects of ethanol, glutamatergic agents have attracted attention for the treatment of ethanol abuse and dependence in preclinical and clinical studies. In the present study, we investigated the effect of pharmacological doses of the natural polyamines putrescine, spermine, and spermidine and the synthetic polyamine N,N'-bis-(3-aminopropyl)cyclohexane-1,4-diamine (DCD) on alcohol consumption in a free-choice paradigm carried out in genetically high-ethanol-consumer UChB rats. Short 3-day treatment with either polyamine, administered p.
View Article and Find Full Text PDFThe aqueous extract obtained from Stichaster striatus Müller & Troschel (Asteroidea, Stichasteridae) has been shown to possess activity as an alcohol appetite inhibitor after oral administration in a rat model with a genetically established excessive appetite for alcohol (Wistar rats, lineage UChB). A significant decrease in the consumption of ethanol was observed (unrelated to a possible disulfiram effect) without a change in the normal food or water intake during the experimentation period. A bio-guided fractionation of the extract was carried out in order to identify the most active fraction, in which the presence of a group of natural endogenous polyamines in undetermined proportions is suspected.
View Article and Find Full Text PDFThis report describes the design and synthesis of the synthetic polyamine DCD (N,N'-bis-(3-aminopropyl)cyclohexane-1,4-diamine, tetramethanesulfonate), a structural analog of spermine, and its in vivo activity as an inhibitor of alcohol consumption in a free-paradigm carried out on genetically high-ethanol-consuming UChB rats. After acute treatment with DCD (daily single dose, 20 mg/kg, p.o.
View Article and Find Full Text PDFThe analgesic effects of (+)- and (-)-amphetamine (AMPH), (+/-)-p-methoxyamphetamine (MA), (+/-)-N-methyl-p-methoxyamphetamine (MMA) and (+/-)-N-ethyl-p-methoxyamphetamine (EMA) were compared using two different algesimetric tests in rats. In the formalin test, (+)-AMPH elicited significant antinociception at doses of 0.2, 2 and 8 mg/kg (i.
View Article and Find Full Text PDFIn rats submitted to a C-fiber reflex response paradigm, intravenous (i.v.) administration of 2.
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