GABA-ergic mechanisms in the anticonvulsive activity of newly-synthesized barbiturates. I. Effects of barbiturates on the convulsive action of GABA-antagonists.
The anticonvulsive activity of seven newly-synthesized derivatives of barbituric acid, having a hydroxylamins groups substituted in second position, with respect to convulsive agents related with the GABA-ergic transmitter system: picrotoxin, bicuculline, thiosemicarbazide and 3-mercaptopropionic acid, was studied in experiments on mice. The anticonvulsive activity of these compounds in allylglycine-induced convulsions was investigated in experiments on rats, and was compared to that of well-known drugs, such as pentobarbital, phenobarbital, allobarbital and diphenylhydantoin. The results obtained show that the hydroxylamine derivatives of barbituric acid HB-2 (2-hydroxylamino-5-ethyl-5-propylbarbituric acid) and HB-7 (2-hydroxylamino-5-ethyl-5 sec. pentylbarbituric acid) have the most pronounced anticonvulsive activity, which suggests the considerable importance of the participation of GABA-ergic transmission in the realization of this activity.
Experimental Pharmacology Departement, Bulgarian Academy of Sciences.
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D
Getova
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V
Georgiev
D015097:3-Mercaptopropionic Acid / Q000037:antagonists & inhibitors; D000501:Allylglycine / Q000037:antagonists & inhibitors; D000818:Animals; D000927:Anticonvulsants; D001463:Barbiturates / Q000494:pharmacology*; D001640:Bicuculline / Q000037:antagonists & inhibitors; D018756:GABA Antagonists; D008297:Male; D051379:Mice; D010852:Picrotoxin / Q000037:antagonists & inhibitors; D051381:Rats; D012640:Seizures / Q000139:chemically induced / Q000517:prevention & control; D012663:Semicarbazides / Q000037:antagonists & inhibitors; D005680:gamma-Aminobutyric Acid / Q000502:physiology*
D015097:3-Mercaptopropionic Acid; D000501:Allylglycine; D000927:Anticonvulsants; D001463:Barbiturates; D001640:Bicuculline; D018756:GABA Antagonists; D010852:Picrotoxin; D012663:Semicarbazides; D005680:gamma-Aminobutyric Acid; C005151:thiosemicarbazide