GABA-ergic mechanisms in the anticonvulsive activity of newly-synthesized barbiturates. I. Effects of barbiturates on the convulsive action of GABA-antagonists.

Abstract

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.

• Authors: D Getova, V Georgiev
• Journal: Acta physiologica et pharmacologica Bulgarica (Acta Physiol Pharmacol Bulg) Vol. 13 Issue 3 Pg. 43-50 ( 1987) ISSN: 0323-9950 [Print] Bulgaria
• PMID: 3439474 (Publication Type: Journal Article)

Chemical References

• Anticonvulsants
• Barbiturates
• GABA Antagonists
• Semicarbazides
• Allylglycine
• Picrotoxin
• gamma-Aminobutyric Acid
• thiosemicarbazide
• 3-Mercaptopropionic Acid
• Bicuculline

Topics

• 3-Mercaptopropionic Acid (antagonists & inhibitors)
• Allylglycine (antagonists & inhibitors)
• Animals
• Anticonvulsants
• Barbiturates (pharmacology)
• Bicuculline (antagonists & inhibitors)
• GABA Antagonists
• Male
• Mice
• Picrotoxin (antagonists & inhibitors)
• Rats
• Seizures (chemically induced, prevention & control)
• Semicarbazides (antagonists & inhibitors)
• gamma-Aminobutyric Acid (physiology)