Design, Synthesis and Biological evaluation of a bivalent μ opiate and adenosine A1 receptors antagonist
Abstract
We designed and synthesized a new hetero-bivalent ligand having 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 bipolar compound increases cAMP production both in cells over expressing the μ receptor and in those over expressing the A1 adenosine receptor and reverses the antalgic effects of μ and A1 adenosine receptors agonist in animals.
Domains
Organic chemistry
Origin : Files produced by the author(s)
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