Effect of SB-205384 on the decay of GABA-activated chloride currents in granule cells cultured from rat cerebellum.
Br J Pharmacol
; 121(7): 1334-8, 1997 Aug.
Article
em En
| MEDLINE
| ID: mdl-9257911
ABSTRACT
1. 4-Amino-7-hydroxy-2-methyl-5,6,7,8,-tetrahydrobenzo[b]thieno[2,3-b]pyrid ine-3-carboxylic acid, but-2-ynyl ester (SB-205384) and other gamma-aminobutyric acid(A) (GABA(A)) receptor modulators were tested for their effects on GABA-activated chloride currents in rat cerebellar granule cells by use of the whole-cell patch clamp technique. 2. The major effect of SB-205384 on GABA(A)-activated current was an increase in the half-life of decay of the response once the agonist had been removed. This is in contrast to many GABA(A) receptor modulators that have previously been shown to potentiate GABA-activated currents. 3. This profile could be explained if SB-205384 stabilizes the channel in open and desensitized states so that channel closing is dramatically slowed. Such a modulatory profile may produce a novel behavioural profile in vivo.
Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Tiofenos
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Cerebelo
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Canais de Cloreto
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Moduladores GABAérgicos
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Ácido gama-Aminobutírico
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Aminopiridinas
Limite:
Animals
Idioma:
En
Ano de publicação:
1997
Tipo de documento:
Article