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Anti-inflammatory Silent Agonists
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2017-09-26 00:00:00 , DOI: 10.1021/acsmedchemlett.7b00368
Nicole A. Horenstein 1 , Roger L. Papke 2
Affiliation  

The traditional view of nicotinic acetylcholine receptors (nAChRs) is that they strictly exert their functions via their well-known ion channel activity. With the identification of the cholinergic anti-inflammatory pathway and the critical involvement of the α7 nAChR, an alternate modality of function has emerged for the receptor involving metabotropic-like activity. The new emerging pharmacology for the receptor includes ligands termed silent agonists, which exert little or no ionotropic activity, yet are capable of modulating cellular inflammatory responses.

中文翻译:

抗炎沉默激动剂

烟碱乙酰胆碱受体(nAChRs)的传统观点是,它们通过众所周知的离子通道活性严格发挥其功能。通过鉴定胆碱能抗炎途径和α7nAChR的关键参与,已经出现了涉及代谢型活性的受体的另一种功能方式。该受体的新药理学包括称为沉默激动剂的配体,其几乎不发挥或不产生离子活性,但能够调节细胞炎症反应。
更新日期:2017-09-26
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