作者:Jing, Lina、Liu, Chunxia
DOI:10.1111/cbdd.14584
日期:——
Transient receptor potential vanilloid 1 (TRPV1) is a non‐selective cation channel, which is considered a highly validated target for pain perception. Repeated activation with agonists to desensitize receptors or use the antagonists can both exert analgesic effects. In this work, two series of novel phenylpiperazine derivatives were designed, synthesized, and evaluated for the in vitro receptor inhibitory
瞬时受体电位香草酸 1 (TRPV1) 是一种非选择性阳离子通道,被认为是经过高度验证的疼痛感知靶点。用激动剂反复激活使受体脱敏或使用拮抗剂都可以发挥镇痛作用。本工作设计、合成了两个系列的新型苯基哌嗪衍生物,并评价了其体外受体抑制活性和体内镇痛活性。其中,含有磺酰脲类的L-21在多种疼痛模型中具有有效的TRPV1拮抗活性和镇痛活性。同时,L-21 表现出低热副作用的风险。这些结果表明,L-21 是进一步开发新型 TRPV1 拮抗剂来治疗疼痛的有希望的候选者。