The Novel, Orally Active, Delta Opioid RWJ-394674 Is Biotransformed to the Potent Mu Opioid RWJ-413216

  title={The Novel, Orally Active, Delta Opioid RWJ-394674 Is Biotransformed to the Potent Mu Opioid RWJ-413216},
  author={Ellen E. Codd and John R. Carson and Raymond W. Colburn and Scott L. Dax and Daksha Desai-Krieger and Rebecca P. Martinez and Linda A. Mckown and Lou Anne Neilson and Philip M. Pitis and Paul L. Stahle and Dennis J. Stone and Anthony J. Streeter and W. N. Wu and S P Zhang},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  pages={1273 - 1279}
  • E. Codd, J. Carson, S. -. Zhang
  • Published 1 September 2006
  • Biology, Chemistry
  • Journal of Pharmacology and Experimental Therapeutics
Although the mu opioid receptor is the primary target of marketed opioid analgesics, several studies suggest the advantageous effect of combinations of mu and delta opioids. The novel compound RWJ-394674 [N,N-diethyl-4-[(8-phenethyl-8-azabicyclo]3.2.1]oct-3-ylidene)-phenylmethyl]-benzamide]; bound with high affinity to the delta opioid receptor (0.2 nM) and with weaker affinity to the mu opioid receptor (72 nM). 5′-O-(3-[35S]-thio)triphosphate binding assay demonstrated its delta agonist… 

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