title: Design, synthesis and biological evaluation of a bivalent micro opiate and adenosine A1 receptor antagonist.
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.
authors.affiliation: Aix-Marseille Université, Institut des Sciences Moléculaires de Marseille, iSm2-UMR CNRS 6263, Centre Saint Jérôme, Service 531, 13397 Marseille Cedex 20, France.
authors.forename: Smitha C
authors.initials: SC
authors.lastname: Mathew
authors.forename: Nandita
authors.initials: N
authors.lastname: Ghosh
authors.forename: Youlet
authors.initials: Y
authors.lastname: By
authors.forename: Aurélie
authors.initials: A
authors.lastname: Berthault
authors.forename: Marie-Alice
authors.initials: MA
authors.lastname: Virolleaud
authors.forename: Louis
authors.initials: L
authors.lastname: Carrega
authors.forename: Gaëlle
authors.initials: G
authors.lastname: Chouraqui
authors.forename: Laurent
authors.initials: L
authors.lastname: Commeiras
authors.forename: Jocelyne
authors.initials: J
authors.lastname: Condo
authors.forename: Mireille
authors.initials: M
authors.lastname: Attolini
authors.forename: Anouk
authors.initials: A
authors.lastname: Gaudel-Siri
authors.forename: Jean
authors.initials: J
authors.lastname: Ruf
authors.forename: Jean-Luc
authors.initials: JL
authors.lastname: Parrain
authors.forename: Jean
authors.initials: J
authors.lastname: Rodriguez
authors.forename: Régis
authors.initials: R
authors.lastname: Guieu
mesh_terms: D000241:Adenosine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D058916:Adenosine A1 Receptor Antagonists; D000813:Anilides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D008024:Ligands; D015394:Molecular Structure; D017450:Receptors, Opioid, mu / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D058916:Adenosine A1 Receptor Antagonists; D000813:Anilides; D008024:Ligands; D017450:Receptors, Opioid, mu; D000241:Adenosine