Synthesis and evaluation of halogenated dibenzodiazepines as muscarinic receptor ligands

Article abstract of DOI:10.1016/S0960-894X(97)00109-1

Syntheses of four novel amide analogues of the muscarinic M₂ receptor antagonists, DIBA and BIBN 140, are described from a common intermediate. Pharmacological evaluation through in vitro assays reveals high muscarinic receptor affinity in each of the compounds, but variable subtype selectivity, primarily M₂ but in one case M₃.