塞来昔布在抑制钙活化氯离子通道ANO1中的新作用

IF 3 3区医学 Q2 PHARMACOLOGY & PHARMACY

Journal of pharmacological sciences Pub Date : 2025-05-02 DOI:10.1016/j.jphs.2025.05.003

Ping Zhou , Qinqin Li , Xiangyu Li , Yani Liu

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引用次数: 0

摘要

塞来昔布是一种非甾体抗炎药，因其通过抑制COX-2而具有镇痛和抗炎作用，被广泛应用于临床。塞来昔布还可调节多种离子通道，包括Nav1.5、Kv7和Kv2.1通道。在这里，我们展示了塞来昔布在抑制钙活化氯离子通道ANO1的新作用，这是参与疼痛感觉。塞来昔布对ANO1电流的抑制呈浓度依赖性，IC50值为20.3±1.9 μM， S7中的残留物P701对塞来昔布介导的ANO1抑制很重要。这些结果表明，ANO1抑制可能有助于塞来昔布的镇痛和抗炎作用。

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A novel role of celecoxib in the inhibition of calcium-activated chloride channel ANO1

Celecoxib, a non-steroidal anti-inflammatory drug, is widely used in the clinic for its analgesic and anti-inflammatory effects by inhibiting COX-2. Celecoxib also modulates many ion channels including Nav1.5, Kv7 and Kv2.1 channels. Here we show a novel role of celecoxib in inhibiting calcium-activated chloride channel ANO1 that is involved in pain sensation. Celecoxib results in a concentration-dependent inhibition of ANO1 current with an IC₅₀ value of 20.3 ± 1.9 μM, and the residue P701 in the S7 is important for celecoxib-mediated ANO1 inhibition. These results suggest that ANO1 inhibition may contribute to celecoxib's analgesic and anti-inflammatory effects.

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来源期刊

Journal of pharmacological sciences 医学-药学

CiteScore

6.20

自引率

2.90%

发文量

104

审稿时长

31 days

期刊介绍： Journal of Pharmacological Sciences (JPS) is an international open access journal intended for the advancement of pharmacological sciences in the world. The Journal welcomes submissions in all fields of experimental and clinical pharmacology, including neuroscience, and biochemical, cellular, and molecular pharmacology for publication as Reviews, Full Papers or Short Communications. Short Communications are short research article intended to provide novel and exciting pharmacological findings. Manuscripts concerning descriptive case reports, pharmacokinetic and pharmacodynamic studies without pharmacological mechanism and dose-response determinations are not acceptable and will be rejected without peer review. The ethnopharmacological studies are also out of the scope of this journal. Furthermore, JPS does not publish work on the actions of biological extracts unknown chemical composition.