Emil Ștefănescu 1, Aurelia Nicoleta Cristea 1, Gabriela Putina 2
1 Faculty of Pharmacy, University of Medicine and Pharmacy Carol Davila – Bucharest
2 Romanian National Institute of Chemical – Pharmaceutical Research and Development – Bucharest
Abstract
A newly synthesized compound by the Romanian National Institute of Chemical-Pharmaceutical Research and Development – Bucharest, conventionally named C1 and belonging to a larger group of substituted phenylethylamines with potential β3 adrenergic properties, was studied in order to determine its selectivity on β adrenergic receptors. Compounds in this class have shown in previous studies the capacity to induce hypoglycemia in normal rats [1] and to have a positive effect on the body mass evolution of normal mice without influencing significantly the food intake[2]. The studied compound has shown intense nervous stimulation, both in the acute toxicity tests as well as in the motor activity evaluation tests. Considering the hypothesis that the central nervous system (CNS) stimulation, observed on administrating compound C1 has a β1 adrenergic receptors agonist mechanism, we investigated whether an antagonism between C1 and propranolol (a well known nonselective β adrenergic receptors antagonist) can be established. For this purpose we used the Actometry test in order to determine the motor behavior and the single dose acute toxicity test in normal mice. Adrenaline and Ephedrine were used as reference substances as they are known to be nonselective α-β adrenergic receptors agonists. Results confirmed the hypothesis, showing a statistically significant decrees in the horizontal motor activity (-22.63%, p<0.001), as well as a significant reduction in mortality (-40%, p<0.0001), when C1 was associated with propranolol. A similar phenomenon was also observed when adrenaline was associated with propranolol. These first results encourage further research in this direction.