VU0255035 is a competitive, orthosteric antagonist of the muscarinic M1 receptor (IC50 = 130 nM). It displays at least 75-fold selectivity for M1 over other muscarinic receptors, as well as a panel of receptors, ion channels, and transporters. VU0255035 is effective in cells and in vivo and brain penetrating, blocking pilocarpine-induced seizures without disrupting contextual fear conditioning in mice. VU0255035 is used to examine the role of the M1 receptor in diverse situations.
