1. Academic Validation
  2. Synthesis and biological evaluation of the major metabolite of atomoxetine: elucidation of a partial kappa-opioid agonist effect

Synthesis and biological evaluation of the major metabolite of atomoxetine: elucidation of a partial kappa-opioid agonist effect

  • Bioorg Med Chem Lett. 2004 Aug 2;14(15):4083-5. doi: 10.1016/j.bmcl.2004.05.018.
Christopher J Creighton 1 Kris Ramabadran Patrick E Ciccone Jingchun Liu Michael J Orsini Allen B Reitz
Affiliations

Affiliation

  • 1 Drug Discovery, Johnson and Johnson Pharmaceutical, Research and Development, Spring House, PA 19477-0776, USA. [email protected]
Abstract

The major human metabolite of atomoxetine (4-hydroxyatomoxetine) was tested against a panel of receptors and Enzymes, and was found to interact with the mu, delta, and kappa-opioid receptors based upon studies involving both binding and functional assays. 4-hydroxyatomoxetine was determined to be a partial agonist of the kappa-opioid receptor.

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