TY - JOUR
T1 - SB 205384 slows the decay of GABA-activated chloride currents in granule cells cultured from rat cerebellum
AU - Meadows, H.J.
AU - Harries, M.
AU - Thompson, M.
AU - Benham, C.D.
N1 - Original article can be found at: http://www.nature.com/bjp/index.html Copyright Nature Publishing Group and British Pharmacological Society. DOI: 10.1038/sj.bjp.0701251 [Full text of this article is not available in the UHRA]
PY - 1997
Y1 - 1997
N2 - 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.
AB - 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.
U2 - 10.1038/sj.bjp.0701251
DO - 10.1038/sj.bjp.0701251
M3 - Article
SN - 0007-1188
VL - 121
SP - 1334
EP - 1338
JO - British Journal of Pharmacology
JF - British Journal of Pharmacology
IS - 7
ER -