Orthosteric ligand affinity

The goal of the investigations, presented here, was to optimize the affinity of the modulators for the common allosteric binding site of muscarinic Mj receptors, the orthosteric site of which was liganded with the antagonist A -methylscolopamine. The phthalimido substituted alkane-bisammonium compound W84 (Fig. 1) was taken as a starting point. 

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