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大麻二酚调节M型钾电流和超极化激活的阳离子电流。

Cannabidiol Modulates M-Type K and Hyperpolarization-Activated Cation Currents.

作者信息

Liu Yen-Chin, So Edmund Cheung, Wu Sheng-Nan

机构信息

Department of Anesthesiology, Kaohsiung Medical University Hospital, Kaohsiung 80756, Taiwan.

Department of Anesthesiology, School of Post-Baccalaureate, College of Medicine, Kaohsiung Medical University, Kaohsiung 80756, Taiwan.

出版信息

Biomedicines. 2023 Sep 27;11(10):2651. doi: 10.3390/biomedicines11102651.

DOI:10.3390/biomedicines11102651
PMID:37893024
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10604323/
Abstract

Cannabidiol (CBD) is a naturally occurring compound found in the plant that is known for its potential therapeutic effects. However, its impact on membrane ionic currents remains a topic of debate. This study aimed to investigate how CBD modifies various types of ionic currents in pituitary GH cells. Results showed that exposure to CBD led to a concentration-dependent decrease in M-type K currents (), with an IC of 3.6 μM, and caused the quasi-steady-state activation curve of the current to shift to a more depolarized potential with no changes in the curve's steepness. The CBD-mediated block of was not reversed by naloxone, suggesting that it was not mediated by opioid receptors. The elicited by pulse-train stimulation was also decreased upon exposure to CBD. The magnitude of -mediated K currents was slightly reduced by adding CBD (10 μM), while the density of voltage-gated Na currents elicited by a short depolarizing pulse was not affected by it. Additionally, CBD decreased the magnitude of hyperpolarization-activated cation currents () with an IC of 3.3 μM, and the decrease was reversed by oxaliplatin. The quasi-steady-state activation curve of was shifted in the leftward direction with no changes in the slope factor of the curve. CBD also diminished the strength of voltage-dependent hysteresis on elicited by upright isosceles-triangular ramp voltage. Collectively, these findings suggest that CBD's modification of ionic currents presented herein is independent of cannabinoid or opioid receptors and may exert a significant impact on the functional activities of excitable cells occurring in vitro or in vivo.

摘要

大麻二酚(CBD)是一种在植物中天然存在的化合物,因其潜在的治疗作用而闻名。然而,其对膜离子电流的影响仍是一个有争议的话题。本研究旨在探究CBD如何改变垂体GH细胞中各种类型的离子电流。结果表明,暴露于CBD会导致M型钾电流()呈浓度依赖性降低,IC为3.6 μM,并使电流的准稳态激活曲线向更去极化的电位移动,而曲线的陡度没有变化。纳洛酮不能逆转CBD介导的对的阻断作用,这表明它不是由阿片受体介导的。暴露于CBD后,脉冲串刺激引发的也减少。添加CBD(10 μM)会使介导的钾电流幅度略有降低,而短去极化脉冲引发的电压门控钠电流密度不受其影响。此外,CBD会降低超极化激活阳离子电流()的幅度,IC为3.3 μM,而奥沙利铂可逆转这种降低。的准稳态激活曲线向左移动,而曲线的斜率因子没有变化。CBD还减弱了由等腰三角形正向斜坡电压引发的对的电压依赖性滞后强度。总的来说,这些发现表明,本文中所述的CBD对离子电流的改变独立于大麻素或阿片受体,可能会对体外或体内可兴奋细胞的功能活动产生重大影响。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2183/10604323/f4b9f271fde2/biomedicines-11-02651-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2183/10604323/c0b792f27c7d/biomedicines-11-02651-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2183/10604323/7fa175956a52/biomedicines-11-02651-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2183/10604323/4e407dd55727/biomedicines-11-02651-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2183/10604323/50ddf0e905fe/biomedicines-11-02651-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2183/10604323/5942737dc52c/biomedicines-11-02651-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2183/10604323/a796521a9c60/biomedicines-11-02651-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2183/10604323/b8a6d00b594d/biomedicines-11-02651-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2183/10604323/f4b9f271fde2/biomedicines-11-02651-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2183/10604323/c0b792f27c7d/biomedicines-11-02651-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2183/10604323/7fa175956a52/biomedicines-11-02651-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2183/10604323/4e407dd55727/biomedicines-11-02651-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2183/10604323/50ddf0e905fe/biomedicines-11-02651-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2183/10604323/5942737dc52c/biomedicines-11-02651-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2183/10604323/a796521a9c60/biomedicines-11-02651-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2183/10604323/b8a6d00b594d/biomedicines-11-02651-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2183/10604323/f4b9f271fde2/biomedicines-11-02651-g008.jpg

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