Multiple ligands applied to dopamine and adenosine receptors

Multivalent ligands are promising pharmacological tools that may be more efficacious for several diseases than highly selective single-target drugs. Here we prepared dual ligands acting on adenosine and dopamine receptors by applying a combinatorial approach based on the ergolene privileged structure. The potency and efficacy of these novel compounds were determined by radioligand binding studies and intracellular cAMP production assays, and selected compounds with dopamine agonist and adenosine antagonist activity were evaluated in vivo. Molecules with this pharmacological profile are potentially useful for studying dopamine-adenosine cross-talk in the central nervous system and for testing the therapeutic potential of multivalent drugs for Parkinson's disease.