2-(2-Phenylcyclopropyl)imidazolines: Reversed Enantioselective Interaction at I1 and I2 Imidazoline Receptors

We have shown that the imidazoline I1 and I2 receptor binding sites have stereospecific requirements, the two subtypes showing a reversal of enatioselectivity, which may offer leads to the development of selective imidazoline receptor ligands. The couple of imidazoline enantiomers (1R,2R)-(-)-4b and (1S,2S)-(+)-4b reported herein, together with other properly designed chiral ligands, may be considered as valid tools for a more extensive eudismic analysis aimed at a necessary subtyping of the I receptors. Work along this line is in progress.