Abstract：
UNASSIGNED: TRPA1 is a nonselective calcium channel, a member of the transient receptor potential (TRP) superfamily, also referred to as the \'irritant\' receptor, being activated by pungent and noxious exogenous chemicals as well as by endogenous algogenic stimuli, to elicit pain, itching, and inflammatory conditions. For this reason, it is considered an attractive therapeutic target to treat a wide range of diseases including acute and chronic pain, itching, and inflammatory airway diseases.
UNASSIGNED: The present review covers patents on TRPA1 antagonists disclosed from 2020 to present, falling in the following main classes: i) novel therapeutic applications for known or already disclosed antagonists, ii) identification and characterization of TRPA1 antagonists from natural sources, and iii) synthesis and evaluation of novel compounds.
UNASSIGNED: Despite the limited number of TRPA1 antagonists in clinical trials, there is an ever-growing interest on this receptor-channel as therapeutic target, mainly due to the relevant outcomes from basic research, which unveiled novel physio-pathological mechanisms where TRPA1 is believed to play a pivotal role, for example the Alzheimer\'s disease or ocular diseases, expanding the panel of potential therapeutic applications for TRPA1 modulators.
UNASSIGNED: The present review covers patents on TRPA1 antagonists disclosed from 2020 to present, falling in the following main classes: i) novel therapeutic applications for known or already disclosed antagonists, ii) identification and characterization of TRPA1 antagonists from natural sources, and iii) synthesis and evaluation of novel compounds.
UNASSIGNED: Despite the limited number of TRPA1 antagonists in clinical trials, there is an ever-growing interest on this receptor-channel as therapeutic target, mainly due to the relevant outcomes from basic research, which unveiled novel physio-pathological mechanisms where TRPA1 is believed to play a pivotal role, for example the Alzheimer\'s disease or ocular diseases, expanding the panel of potential therapeutic applications for TRPA1 modulators.
摘要：
■TRPA1是一种非选择性钙通道，瞬时受体电位（TRP）超家族的成员，也称为“刺激物”受体，被刺激性和有害的外源性化学物质以及内源性的藻类刺激激活，引发疼痛，瘙痒和炎症条件。出于这个原因,它被认为是一个有吸引力的治疗目标，以治疗广泛的疾病，包括急性和慢性疼痛，痒,和炎症性气道疾病。
■本综述涵盖了从2020年至今公开的TRPA1拮抗剂的专利，属于以下主要类别:i)已知或已经公开的拮抗剂的新治疗应用，ii）来自天然来源的TRPA1拮抗剂的鉴定和表征，和iii)新化合物的合成和评价。
■尽管临床试验中TRPA1拮抗剂的数量有限，人们对这种受体通道作为治疗靶标的兴趣越来越大，主要是由于基础研究的相关成果，揭示了新的生理病理机制的鉴定，其中TRPA1被认为起着关键作用，例如阿尔茨海默病或眼病，扩大TRPA1调节剂的潜在治疗应用小组。
■本综述涵盖了从2020年至今公开的TRPA1拮抗剂的专利，属于以下主要类别:i)已知或已经公开的拮抗剂的新治疗应用，ii）来自天然来源的TRPA1拮抗剂的鉴定和表征，和iii)新化合物的合成和评价。
■尽管临床试验中TRPA1拮抗剂的数量有限，人们对这种受体通道作为治疗靶标的兴趣越来越大，主要是由于基础研究的相关成果，揭示了新的生理病理机制的鉴定，其中TRPA1被认为起着关键作用，例如阿尔茨海默病或眼病，扩大TRPA1调节剂的潜在治疗应用小组。
