Victoriano Darias

Synthesis and preliminary pharmacological evaluation of thiophene analogues of viloxazine as potentialantidepressant drugs

A series of eight thienyloxymethylmorpholines, thiophene analogues of viloxazine, have been synthesized by three different routes. The preliminary pharmacological evaluation of this series shows antidepressant properties on the mice models used with a light sedative action. The structure-activity relationship is established in a first approximation.

Neuropharmacological study of hetero[2,1]benzothiazepine derivatives analogues of tianeptine

Neuropharmacological studies were conducted in mice with a number of hetero[2,1]benzothiazepine derivatives, analogues of tianeptine. Seven of the 12 compounds under study potentiated the actions of 5-hydroxytryptophan (5-HTP, 50 mg/kg i.p.) and/or antagonised the hypothermia induced by high doses of apomorphine. Moreover, some of them inhibited the head twitches induced by 5-HTP (250 mg/kg i.p.) and the stereotyped behaviour and/or climbing behaviour of low doses of apomorphine. These compounds also produced a slight inhibition of exploratory behaviour in the holeboard test. On the other hand, no significant muscle relaxant, anticonvulsant and anxiolytic activities were observed at any dose employed. Together, these data suggest that some of the compounds under study exert antidepressant and neuroleptic effects in mice with no muscle relaxant, anxiolytic and anticonvulsant activities.

5,6-Dihydro-1H,4H-pyrazolo[4,3-f]pyrrolo[1,2-a][1,4]diazepines. Synthesis and pharmacological evaluation

Abstract A series of new 5,6 dihydro-1H,4H-pyrazolo[4,3-f]pyrrolo[1,2-a][1,4]diazepines was synthesized and tested for acute toxicity and CNS activity in mice. Some of these compounds were shown to possess anxiolytic activity similar to that of diazepam, with weak anticonvulsant and sedative action.

Study of the Hypoglycaemic, Diuretic and Cardiovascular Activity of Cedronella canariensis var. canariensis (L.) W. & B.

The hypoglycaemic, diuretic and cardiovascular activities of an infusion and CHCl3 extract of the aerial part of Cedronella canariensis (L.) Webb & Berth are presented. It was observed that the CHCl3 extract had a significant hypoglycaemic and diuretic effect. At the cardiovascular level, the infusion and CHCl3 extract exercised a marked hypotensor effect in vivo and a brachycardiac activity in the isolated atria of the rat.