Synthesis and pharmacological study of some new beta-(dialkylaminomethyl)- gamma-butyrolactones and their tetrahydrofuran analogues.
This paper describes the synthesis of beta-(dialkylaminomethyl)-gamma- butyrolactones (6 and 15) and their tetrahydrofuran analogs 7 and 16. Their convulsant activity was studied on mice and could display an antiGABAergic component, but, unlike the alpha-(dialkylaminomethyl)- gamma-butyrolactones, no antiglycinergic component was detected. The possibility of an activation of the glutamatergic receptors (NMDA), by indirect stimulation of their glycinergic site, by the tetrahydrofurans analogs 7 could be considered. These compounds exhibited, at low doses (1/3 to 1/20 of their convulsant doses), an anticonvulsant action in the maximal electroshock test and this is in agreement with the abovementioned possibility.
Foscolos
G B
GB
Department of Pharmacy, University of Athens, Greece.
Kolocouris
N
N
Fytas
G
G
Marakos
P
P
Pouli
N
N
Vamvakides
A
A
D015107:4-Butyrolactone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D001285:Atropine / Q000494:pharmacology; D003292:Convulsants / Q000138:chemical synthesis* / Q000494:pharmacology; D004830:Epilepsy, Tonic-Clonic / Q000139:chemically induced; D018690:Excitatory Amino Acid Agonists / Q000138:chemical synthesis* / Q000494:pharmacology; D018684:Glycine Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D051379:Mice; D008814:Mice, Inbred NZB; D018727:Muscarinic Antagonists / Q000494:pharmacology; D051381:Rats
D003292:Convulsants; D018690:Excitatory Amino Acid Agonists; D018684:Glycine Agents; D018727:Muscarinic Antagonists; D001285:Atropine; D015107:4-Butyrolactone