BS46 is a highly potent and selective muscarinic acetylcholine receptor antagonist that exhibits 33-fold preference for M3R (M3 muscarinic acetylcholine receptor) over M2R. It fully inhibits carbachol-induced inositol monophosphate accumulation as well as ?-arrestin recruitment at M3Rs. BS46 exhibits 100,000-fold selectivity for muscarinic receptors against 21 aminergic and peptidergic GPCRs.
highly potent and selective M3 muscarinic acetylcholine receptor (M3R) antagonist that exhibits 33-fold preference for M3R over M2R
Proceedings of the National Academy of Sciences of the United States of America, 115(47), 12046-12050 (2018-11-09)
Drugs that treat chronic obstructive pulmonary disease by antagonizing the M3 muscarinic acetylcholine receptor (M3R) have had a significant effect on health, but can suffer from their lack of selectivity against the M2R subtype, which modulates heart rate. Beginning with
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