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Doc ID CHEMBL1154631
Journal Bioorg Med Chem Lett (2009) 19:6736-6739
Title Design, synthesis and biological evaluation of a bivalent micro opiate and adenosine A1 receptor antagonist.
Authors Mathew SC, Ghosh N, By Y, Berthault A, Virolleaud MA, Carrega L, Chouraqui G, Commeiras L, Condo J, Attolini M, Gaudel-Siri A, Ruf J, Parrain JL, Rodriguez J, Guieu R.
Abstract 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 A(1) adenosine and mu opiate receptors with a K(i) of 0.8+/-0.05 and 0.7+/-0.03 microM, respectively. This hybrid molecule increases cAMP production in cells that over express the mu receptor as well as those over expressing the A(1) adenosine receptor and reverses the antalgic effects of mu and A(1) adenosine receptor agonists in animals.
CiteXplore 19836950
DOI 10.1016/j.bmcl.2009.09.112

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