BS46 is a highly potent and selective muscarinic acetylcholine receptor antagonist th at 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.