Discovery of non-peptide, small molecule antagonists of α9α10 nicotinic acetylcholine receptors as novel analgesics for the treatment of neuropathic a...
Basic Information
ID: ALA1759897
Journal: Bioorg Med Chem Lett
Title: Discovery of non-peptide, small molecule antagonists of α9α10 nicotinic acetylcholine receptors as novel analgesics for the treatment of neuropathic and tonic inflammatory pain.
Authors: Zheng G, Zhang Z, Dowell C, Wala E, Dwoskin LP, Holtman JR, McIntosh JM, Crooks PA.
Abstract: A 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.
CiteXplore: 21397497
DOI: 10.1016/j.bmcl.2011.02.043
Patent ID: ┄