NS 1619 activates BKCa channel activity in rat cortical neurones

Kevin Lee; I C Rowe; M L Ashford

doi:10.1016/0014-2999(95)00251-F

NS 1619 activates BKCa channel activity in rat cortical neurones

Kevin Lee, I C Rowe, M L Ashford

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

39 Citations (Scopus)

Abstract

Single channel recordings of large conductance Ca2(+)-activated K+ (BKCa) channels were made from neurones isolated from rat motor cortex. Application of levcromakalim, pinacidil or diazoxide had no effect on BKCa channel activity in excised patches. In contrast, NS 1619 (1-(2'-hydroxy-5'-trifluoromethylphenyl)-5-trifluoromethyl- 2(3H)benzimidazalone) induced concentration-dependent activation of BKCa channels with a calculated EC50 of 32 microM. The NS 1619-induced activity was dependent on the presence of free Ca2+ at the intracellular surface, but was not associated with a change in channel voltage sensitivity. Niflumic acid had no effect on BKCa activity per se but prevented NS 1619-mediated activation.

Original language	English
Pages (from-to)	215-9
Number of pages	5
Journal	European Journal of Pharmacology
Volume	280
Issue number	2
DOIs	https://doi.org/10.1016/0014-2999(95)00251-F
Publication status	Published - 4 Jul 1995

Keywords

Rats
Motor Cortex
Benzimidazoles
Animals
Rats, Sprague-Dawley
Calcium
Neurons
Adenosine Triphosphate
Potassium Channels
Male

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10.1016/0014-2999(95)00251-F

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title = "NS 1619 activates BKCa channel activity in rat cortical neurones",

abstract = "Single channel recordings of large conductance Ca2(+)-activated K+ (BKCa) channels were made from neurones isolated from rat motor cortex. Application of levcromakalim, pinacidil or diazoxide had no effect on BKCa channel activity in excised patches. In contrast, NS 1619 (1-(2'-hydroxy-5'-trifluoromethylphenyl)-5-trifluoromethyl- 2(3H)benzimidazalone) induced concentration-dependent activation of BKCa channels with a calculated EC50 of 32 microM. The NS 1619-induced activity was dependent on the presence of free Ca2+ at the intracellular surface, but was not associated with a change in channel voltage sensitivity. Niflumic acid had no effect on BKCa activity per se but prevented NS 1619-mediated activation.",

keywords = "Rats, Motor Cortex, Benzimidazoles, Animals, Rats, Sprague-Dawley, Calcium, Neurons, Adenosine Triphosphate, Potassium Channels, Male",

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year = "1995",

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doi = "10.1016/0014-2999(95)00251-F",

language = "English",

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TY - JOUR

T1 - NS 1619 activates BKCa channel activity in rat cortical neurones

AU - Lee, Kevin

AU - Rowe, I C

AU - Ashford, M L

PY - 1995/7/4

Y1 - 1995/7/4

N2 - Single channel recordings of large conductance Ca2(+)-activated K+ (BKCa) channels were made from neurones isolated from rat motor cortex. Application of levcromakalim, pinacidil or diazoxide had no effect on BKCa channel activity in excised patches. In contrast, NS 1619 (1-(2'-hydroxy-5'-trifluoromethylphenyl)-5-trifluoromethyl- 2(3H)benzimidazalone) induced concentration-dependent activation of BKCa channels with a calculated EC50 of 32 microM. The NS 1619-induced activity was dependent on the presence of free Ca2+ at the intracellular surface, but was not associated with a change in channel voltage sensitivity. Niflumic acid had no effect on BKCa activity per se but prevented NS 1619-mediated activation.

AB - Single channel recordings of large conductance Ca2(+)-activated K+ (BKCa) channels were made from neurones isolated from rat motor cortex. Application of levcromakalim, pinacidil or diazoxide had no effect on BKCa channel activity in excised patches. In contrast, NS 1619 (1-(2'-hydroxy-5'-trifluoromethylphenyl)-5-trifluoromethyl- 2(3H)benzimidazalone) induced concentration-dependent activation of BKCa channels with a calculated EC50 of 32 microM. The NS 1619-induced activity was dependent on the presence of free Ca2+ at the intracellular surface, but was not associated with a change in channel voltage sensitivity. Niflumic acid had no effect on BKCa activity per se but prevented NS 1619-mediated activation.

KW - Rats

KW - Motor Cortex

KW - Benzimidazoles

KW - Animals

KW - Rats, Sprague-Dawley

KW - Calcium

KW - Neurons

KW - Adenosine Triphosphate

KW - Potassium Channels

KW - Male

U2 - 10.1016/0014-2999(95)00251-F

DO - 10.1016/0014-2999(95)00251-F

M3 - Article

C2 - 7589189

SN - 0014-2999

VL - 280

SP - 215

EP - 219

JO - European Journal of Pharmacology

JF - European Journal of Pharmacology

IS - 2

ER -

NS 1619 activates BKCa channel activity in rat cortical neurones

Abstract

Keywords

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