TRPA1 inhibitors-5(University of Eastern Finland)(TRPA1 inhibitors-5(University of Eastern Finland)) - 药物靶点：TRPA1_在研适应症：炎症，疼痛_专利_临床

概要

基本信息

药物类型

小分子化药

别名-

靶点

TRPA1

作用方式

抑制剂

作用机制

TRPA1抑制剂(瞬时受体电位离子通道亚基1抑制剂)

治疗领域

神经系统疾病其他疾病

在研适应症

炎症疼痛

非在研适应症-

原研机构-

在研机构

University of Eastern Finland

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 TRPA1 inhibitors-5(University of Eastern Finland) 相关的临床结果

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100 项与 TRPA1 inhibitors-5(University of Eastern Finland) 相关的转化医学

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100 项与 TRPA1 inhibitors-5(University of Eastern Finland) 相关的专利（医药）

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1

项与 TRPA1 inhibitors-5(University of Eastern Finland) 相关的文献（医药）

2024-08-08·ACS Medicinal Chemistry Letters

TRPA1 Inhibition Effects by 3-Phenylcoumarin Derivatives

Article

作者: Rahnasto-Rilla, Minna ; Hiltunen, Sanna ; Hämäläinen, Mari ; Lahtela-Kakkonen, Maija ; Timonen, Juri M ; Johansson, Niklas G ; Moilanen, Eeva ; Nousiainen, Liisa P ; Awolade, Paul ; Turhanen, Petri ; Sallomy, Carita

Transient receptor potential ankyrin 1 (TRPA1) protein plays an important role in the inflammatory response, and it has been associated with different pain conditions and pain-related diseases, making TRPA1 a valid target for painkillers. In this study, we identified potential TRPA1 inhibitors and located their binding sites utilizing computer-aided drug design (CADD) techniques. The designed 3-phenylcoumarin-based TRPA1 inhibitors were successfully synthesized using a microwave assisted synthetic strategy. 3-(3-Bromophenyl)-7-acetoxycoumarin (5), 7-hydroxy-3-(3-hydroxyphenyl)coumarin (12) and 3-(3-hydroxyphenyl)coumarin (23) all showed inhibitory activity toward TRPA1 in vitro. Compound 5 also decreased the size and formation of breast cancer cells. Hence, targeting TRPA1 may represent a promising alternative for the treatment of pain and inflammation.

100 项与 TRPA1 inhibitors-5(University of Eastern Finland) 相关的药物交易

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