1202519-15-0Relevant articles and documents
Design, synthesis and biological evaluation of a bivalent μ opiate and adenosine A1 receptor antagonist
Mathew, Smitha C.,Ghosh, Nandita,By, Youlet,Berthault, Aurelie,Virolleaud, Marie-Alice,Carrega, Louis,Chouraqui, Gaelle,Commeiras, Laurent,Condo, Jocelyne,Attolini, Mireille,Gaudel-Siri, Anouk,Ruf, Jean,Parrain, Jean-Luc,Rodriguez, Jean,Guieu, Regis
, p. 6736 - 6739 (2009)
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.
