Design, synthesis and biological evaluation of a bivalent micro opiate and adenosine A1 receptor antagonist.

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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

Design, synthesis and biological evaluation of a bivalent micro opiate and adenosine A1 receptor antagonist.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6736-9. doi: 10.1016/j.bmcl.2009.09.112. Epub 2009 Oct 3.

PubMed ID

19836950 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Naloxone	Mu-type opioid receptor	Ki (nM)	1.5	N/A	N/A	Details