SB 205384 slows the decay of GABA-activated chloride currents in granule cells cultured from rat cerebellum

H.J. Meadows; M. Harries; M. Thompson; C.D. Benham

doi:10.1038/sj.bjp.0701251

SB 205384 slows the decay of GABA-activated chloride currents in granule cells cultured from rat cerebellum

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

Research output: Contribution to journal › Article › peer-review

8 Citations (Scopus)

Abstract

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.

Original language	English
Pages (from-to)	1334-1338
Journal	British Journal of Pharmacology
Volume	121
Issue number	7
DOIs	https://doi.org/10.1038/sj.bjp.0701251
Publication status	Published - 1997

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@article{47be58e95c5248c9842249b21b8d03d6,

title = "SB 205384 slows the decay of GABA-activated chloride currents in granule cells cultured from rat cerebellum",

abstract = "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.",

author = "H.J. Meadows and M. Harries and M. Thompson and C.D. Benham",

note = "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]",

year = "1997",

doi = "10.1038/sj.bjp.0701251",

language = "English",

volume = "121",

pages = "1334--1338",

journal = "British Journal of Pharmacology",

issn = "0007-1188",

publisher = "Wiley-Blackwell",

number = "7",

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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 -

SB 205384 slows the decay of GABA-activated chloride currents in granule cells cultured from rat cerebellum

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