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Effect of SB-205384 on the Decay of GABA-activated Chloride Currents in Granule Cells Cultured From Rat Cerebellum

Effect of SB-205384 on the Decay of GABA-activated Chloride Currents in Granule Cells Cultured From Rat Cerebellum

H J Meadows, M H Harries, M Thompson, C D Benham

Br J Pharmacol. 1997 Aug;121(7):1334-8.

PMID: 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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP160296139	SB 205384		160296-13-9	Price

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