Effect of GABA analogues on various components of maximum electroshock-induced seizures in mice.
Indian J Exp Biol
;
1994 Mar; 32(3): 218-20
Artigo
em Inglês
| IMSEAR
| ID: sea-57223
ABSTRACT
Out of fourteen compounds reported here only four [N-valproyl GABA (V.GABA), N-phthaloyl GABA (P.GABA), gamma-phthalimido N-amyl butyramide (PGA) and gamma-phthalimido N-phenyl butyramide (PGP)] gave significant protection to all the four components of maximal electroshock-induced seizures (MES) in mice. It appeared that substitution of either amino or carboxylic or both groups of gamma-aminobutyric acid (GABA) with bulkier groups like aliphatic or aromatic carbons usually produced effective anticonvulsant GABA derivatives. V.GABA and P.GABA were the most effective anticonvulsant GABA derivatives in protecting all the components of MES-induced seizures. They were 2.3 and 1.5 times potent than sodium valproate in molar ratio, but P.GABA has low therapeutic index when compared to V.GABA. The observed anticonvulsant activity may be due to enhanced GABA concentration in the CNS. Probably, the active compound (V.GABA) crossed the blood brain barrier and hydrolysed to GABA and valproic acid to bring about its anticonvulsant action.
Texto completo:
DisponíveL
Índice:
IMSEAR (Sudeste Asiático)
Assunto principal:
Ratos
/
Convulsões
/
Relação Estrutura-Atividade
/
Barreira Hematoencefálica
/
Eletrochoque
/
Ácido gama-Aminobutírico
/
Animais
/
Camundongos
/
Anticonvulsivantes
Idioma:
Inglês
Revista:
Indian J Exp Biol
Ano de publicação:
1994
Tipo de documento:
Artigo
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