瞬时受体电位通道
化学
TRPV1型
TRPV4型
TRPV公司
药理学
敌手
离子通道
TRPM8型
受体
生物化学
生物
作者
Lili Wang,Ling Zhang,Rongfeng Liu,Yimei Xu,Zhifeng Tang,Congxiao Zhang,Zhong-Yin Zhang
标识
DOI:10.1016/j.bmcl.2023.129577
摘要
Transient receptor potential vanilloid 3 (TRPV3) channel is a temperature-sensitive and Ca2+-permeable nonselective cation channel, which is abundantly expressed in skin keratinocyte and plays an important role in skin homeostasis and repair. However, only a few TRPV3 inhibitors were reported. Few selective and potent modulators of the TRPV3 channel have hindered the progress of the investigation and clinical application. TRPV3 channel research still faces challenges and requires the new inhibitors. Flavonoids are a kind of natural compounds with various biological and pharmacological activities including anti-inflammatory and anti allergic effects, which is associated with some physiological effects mediated by TRPV3 channel. Herein, our group designed and synthesized a range of flavone derivatives, and investigated their inhibitory properties on the human TRPV3 channel by electrophysiology technique. Then, we identified a new potent TRPV3 antagonist 2d with IC50 of 0.62 μM. It also showed good selectivity on TRPV1, TRPV4, TRPA1 and TRPM8.
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