國家衛生研究院 NHRI:Item 3990099045/10247
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    题名: Stimulatory actions of a novel thiourea derivative on large-conductance, calcium-activated potassium channels
    作者: Wu, SN;Chern, JH;Shen, S;Chen, HH;Hsu, YT;Lee, CC;Chan, MH;Lai, MC;Shie, FS
    贡献者: Center for Neuropsychiatric Research;Institute of Biotechnology and Pharmaceutical Research
    摘要: AIM: In this study, we examine whether an anti-inflammatory thiourea derivative, compound #326, actions on ion channels. METHODS: The effects of compound #326 on Ca2+ -activated K+ channels were evaluated by patch-clamp recordings obtained in cell-attached, inside-out or whole-cell configuration. RESULTS: In pituitary GH3 cells, compound #326 increased the amplitude of Ca2+ -activated K+ currents (IK(Ca) ) with an EC50 value of 11.6 muM, which was reversed by verruculogen, but not tolbutamide or TRAM-34. Under inside-out configuration, a bath application of compound #326 raised the probability of large-conductance Ca2+ -activated K+ (BKCa ) channels. The activation curve of BKCa channels was shifted to less depolarised potential with no modification of the gating charge of the curve; consequently, the difference of free energy was reduced in the presence of this compound. Compound #326-stimulated activity of BKCa channels is explained by a shortening of mean closed time, despite its inability to alter single-channel conductance. Neither delayed-rectifier nor erg-mediated K+ currents was modified. Compound #326 decreased the peak amplitude of voltage-gated Na+ current with no clear change in the overall current-voltage relationship of this current. In HEK293T cells expressing alpha-hSlo, compound #326 enhanced BKCa channels effectively. Intriguingly, the inhibitory actions of compound #326 on interleukin 1beta in lipopolysaccharide-activated microglia were significantly reversed by verruculogen, whereas BKCa channel inhibitors suppressed the expressions of inducible nitric oxide synthase. CONCLUSION: The BKCa channels could be an important target for compound #326 if similar in vivo results occur, and the multi-functionality of BKCa channels in modulating microglial immunity merit further investigation. This article is protected by copyright. All rights reserved.
    日期: 2017-12
    關聯: Journal of Cellular Physiology. 2017 Dec;232(12):3409-3421.
    Link to: http://dx.doi.org/10.1002/jcp.25788
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0021-9541&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000408155100020
    Cited Times(Scopus): https://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85017423311
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