Molecules to Selectively Target Receptors for Treatment of Pain and Neurogenic Inflammation
Molecules to Selectively Target Receptors for Treatment of Pain and Neurogenic Inflammation
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DOI：
10.2174/187221312798889266
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发表时间：
2012-01-01
影响因子：
4.2
通讯作者：
Kozlov, Sergey A.
中科院分区：
文献类型：
--
作者：
Andreev, Yaroslav A.;Vassilevski, Alexander A.;Kozlov, Sergey A.
参与疼痛信号产生和传导的受体引起了科学界和企业界的极大兴趣。成功开发有效镇痛药物的良好商业前景极大地刺激了研究。本文提供了一个简单的概述的关键分子靶点，即细胞受体，抑制它可以导致镇痛。目前，瞬时受体电位（TRP）、嘌呤能（P2 X）受体和酸敏感离子通道（ASIC）被认为是感知疼痛刺激的最重要的蛋白质。这些离子型受体也参与炎症的发展;它们的过度活跃导致许多病理状况，并与急性和炎性疼痛密切相关。本文综述了能够选择性调节这些受体的分子的发展，它们在体外和体内的作用，以及专利和研究文章中描述的实际应用前景。
Receptors that are involved in generation and transduction of pain signals attract much interest from the scientific and corporate communities. Good commercial prospects for successful development of effective analgesic drugs stimulate significantly the research. This article provides a brief overview of the key molecular targets, i.e. cell receptors, inhibition of which can lead to analgesia. Today transient receptor potential (TRP), purinergic (P2X) receptors and acid-sensing ion channels (ASIC) are considered to be the most important proteins for perception of pain stimuli. These ionotropic receptors also participate in the development of inflammation; their hyperactivity leads to many pathological conditions and is closely associated with acute and inflammatory pain. Development of molecules capable to selectively modulate these receptors, their in vitro and in vivo effects, as well as perspectives for practical application described in patents and research articles are reviewed in this paper.