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Bioorg. Med. Chem. Lett. · Apr 2011
Discovery of non-peptide, small molecule antagonists of α9α10 nicotinic acetylcholine receptors as novel analgesics for the treatment of neuropathic and tonic inflammatory pain.
- Guangrong Zheng, Zhenfa Zhang, Cheryl Dowell, Elzbieta Wala, Linda P Dwoskin, Joseph R Holtman, J Michael McIntosh, and Peter A Crooks.
- College of Pharmacy, Department of Pharmaceutical Sciences, University of Kentucky, Lexington, KY 40536 0082, USA.
- Bioorg. Med. Chem. Lett. 2011 Apr 15;21(8):2476-9.
AbstractA series of azaaromatic quaternary ammonium analogs has been discovered as potent and selective α9α10 nicotinic acetylcholine receptor (nAChR) antagonists. The preliminary structure-activity relationships of these analogs suggest that increased rigidity in the linker units results in higher potency in inhibition of α9α10 nAChRs and greater selectivity over α7 nAChRs. These analogs represent a new class of analgesic for the treatment of neuropathic and tonic inflammatory pain.Copyright © 2011 Elsevier Ltd. All rights reserved.
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