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血管紧张素 II 型受体:治疗神经性疼痛的新的临床验证靶点。

Angiotensin II type 2-receptor: new clinically validated target in the treatment of neuropathic pain.

机构信息

Department of Surgery and Cancer, Imperial College London, London, SW10 9NH, UK.

出版信息

Clin Pharmacol Ther. 2015 Feb;97(2):128-30. doi: 10.1002/cpt.29. Epub 2014 Dec 20.

Abstract

Neuropathic pain is a large unmet medical need. The angiotensin II type 2 (AT2 ) receptor is a target with promising data in rodent models of peripheral neuropathic pain. The AT2 receptor has attracted attention on the basis of human data from a proof-of-concept clinical trial showing that oral EMA401, a highly selective, peripherally restricted, small molecule AT2 receptor antagonist, at 100 mg twice-daily for 4 weeks, alleviated postherpetic neuralgia, an often intractable type of peripheral neuropathic pain.

摘要

神经性疼痛是一个巨大的未满足的医学需求。血管紧张素 II 型 2(AT2)受体是一个有前途的靶点,在周围神经性疼痛的啮齿动物模型中具有良好的数据。基于一项概念验证临床试验的人类数据,AT2 受体引起了人们的关注,该试验表明,高选择性、外周受限的小分子 AT2 受体拮抗剂 EMA401 口服,每日两次,每次 100 毫克,持续 4 周,可缓解带状疱疹后神经痛,这是一种常见的难治性周围神经性疼痛。

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