Synthesis, physicochemical and conformational properties of (3R,4R)-3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-1-azabicyclo[2.2.1]heptane, a novel M1 selective muscarinic partial agonist

Abstract

The cyclopropyloxadiazole derivative described in the title has been shown to be a functionally selective M₁ partial agonist with antagonist properties in M₂ and M₃ muscarinic receptor assays; conformational studies indicate free rotation around the oxadiazole–azanorbornane bond, whilst X-ray studies reveal that the cyclopropyl group is in conjugation with the oxadiazole CN bond.