Article date: July 1997
By: H J Meadows, M H Harries, M Thompson, C D Benham, in Volume 121, Issue 7, pages 1334-1338
4‐Amino‐7‐hydroxy‐2‐methyl‐5,6,7,8,‐tetrahydrobenzo[b]thieno[2,3‐b]pyridine‐3‐carboxylic acid, but‐2‐ynyl ester (SB‐205384) and other γ‐aminobutyric acidA (GABAA) 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.
The major effect of SB‐205384 on GABAA‐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 GABAA receptor modulators that have previously been shown to potentiate GABA‐activated currents.
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.
4‐Amino‐7‐hydroxy‐2‐methyl‐5,6,7,8,‐tetrahydrobenzo[b]thieno[2,3‐b]pyridine‐3‐carboxylic acid, but‐2‐ynyl ester (SB‐205384) and other γ‐aminobutyric acidA (GABAA) 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.
The major effect of SB‐205384 on GABAA‐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 GABAA receptor modulators that have previously been shown to potentiate GABA‐activated currents.
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.
DOI: 10.1038/sj.bjp.0701251
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