Design, Synthesis and Biological evaluation of a bivalent μ opiate and adenosine A1 receptors antagonist
Résumé
The cross talk between different membrane receptors is the source of increasing research. We designed and synthesized a new hetero-bivalent ligand that has antagonist properties on both A1 adenosine and μ opiate receptors with a Ki of 0.8 ± 0.05 and 0.7 ± 0.03 μM, respectively. This hybrid molecule increases cAMP production in cells that over express the μ receptor as well as those over expressing the A1 adenosine receptor and reverses the antalgic effects of μ and A1 adenosine receptor agonists in animals.