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ACS Med Chem Lett. 2017 Sep 26;8(10):989-991. doi: 10.1021/acsmedchemlett.7b00368. eCollection 2017.

Anti-inflammatory Silent Agonists.

Author information

  • 1Department of Chemistry, University of Florida, Gainesville, Florida 32611-7200, United States.
  • 2Department of Pharmacology and Therapeutics, University of Florida, Gainesville, Florida 32610-0267, United States.

Abstract

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.

PMID:
29057037
PMCID:
PMC5641964
[Available on 2018-10-12]
DOI:
10.1021/acsmedchemlett.7b00368
[PubMed]
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