Synthesis and study of the convulsant action of polycyclic amino-gamma-lactone and of its tetrahydrofuran analogue
Kolocouris, N.; Foscolos, G.B.; Fytas, G.; Vamvakides, A.
Annales Pharmaceutiques Francaises 47(3): 126-134
1989
ISSN/ISBN: 0003-4509 PMID: 2634928 Document Number: 330225
In this paper, the synthesis of the gamma-benzyl-amino-gamma-lactone 6 and its tetrahydrofuran analogue 8 is described. Their convulsant action was studied in mice. They display a weak convulsant activity coming with sedation and myorelaxation. The introduction of the benzyl group abolishes the strong convulsant and lethal action characteristic of the already studied non benzylated aminolactones but leaves intact the aminoethers activity. These results could indicate that the activity of these amino-gamma-lactones is essentially antiglycinergic and those of the corresponding aminoethers is anti-GABAergic lined with a partial agonist action.