Design, Synthesis and Biological evaluation of a bivalent μ opiate and adenosine A1 receptors antagonist - Aix-Marseille Université Access content directly
Journal Articles Bioorganic and Medicinal Chemistry Letters Year : 2009

Design, Synthesis and Biological evaluation of a bivalent μ opiate and adenosine A1 receptors antagonist

Smitha C. Mathew
  • Function : Author
Nandita Ghosh
  • Function : Author
Aurélie Berthault
  • Function : Author
Marie-Alice Virolleaud
Gaëlle Chouraqui
  • Function : Author
Laurent Commeiras
Jean-Luc Parrain
  • Function : Correspondent author
  • PersonId : 921804

Connectez-vous pour contacter l'auteur
Jean Rodriguez
  • Function : Correspondent author
  • PersonId : 921781

Connectez-vous pour contacter l'auteur

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.
Fichier principal
Vignette du fichier
HAL11.pdf (448.79 Ko) Télécharger le fichier
Origin : Files produced by the author(s)
Loading...

Dates and versions

hal-00679622 , version 1 (16-03-2012)

Identifiers

Cite

Smitha C. Mathew, Nandita Ghosh, Youlet By, Aurélie Berthault, Marie-Alice Virolleaud, et al.. Design, Synthesis and Biological evaluation of a bivalent μ opiate and adenosine A1 receptors antagonist. Bioorganic and Medicinal Chemistry Letters, 2009, 19, pp.6736-6739. ⟨10.1016/j.bmcl.2009.09.112⟩. ⟨hal-00679622⟩

Relations

470 View
326 Download

Altmetric

Share

Gmail Facebook Twitter LinkedIn More