[Synthesis and study of the convulsant action of polycyclic amino-gamma-lactone and of its tetrahydrofuran analogue].
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.
Kolocouris
N
N
Foscolos
G B
GB
Fytas
G
G
Vamvakides
A
A
D000818:Animals; D003292:Convulsants / Q000138:chemical synthesis* / Q000494:pharmacology; D004112:Dimercaprol / Q000138:chemical synthesis / Q000494:pharmacology*; D005260:Female; D005663:Furans / Q000138:chemical synthesis / Q000494:pharmacology*; D051379:Mice; D008807:Mice, Inbred BALB C; D009281:Naphthalenes / Q000138:chemical synthesis / Q000494:pharmacology*; D013764:Tetrahydronaphthalenes / Q000138:chemical synthesis / Q000494:pharmacology*
D003292:Convulsants; D005663:Furans; D009281:Naphthalenes; D013764:Tetrahydronaphthalenes; D004112:Dimercaprol; C063935:3-benzyl-1-(dimethylaminomethyl)-3,4,5,9-tetranaphtho(2-1b)(2-1H)-furanone; C063936:3-benzyl-1-(dimethylaminomethyl)-1,2,3,4,5,9-hexahydronaphtho(2-1b)furan
Synthèse et étude de l'action convulsivante d'une amino-gamma-lactone polycyclique et de son analogue tétrahydrofurannique.