Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).

@article{Bourdonnec2008PotentOB,
  title={Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).},
  author={Bertrand Le Bourdonnec and Rolf T. Windh and Christopher W Ajello and Lara K Leister and Minghua Gu and Guo-Hua Chu and Paul A Tuthill and William M Barker and Michael Koblish and Daniel D Wiant and Thomas M. Graczyk and Serge Belanger and Joel A Cassel and Marina S Feschenko and Bernice L Brogdon and Steven A Smith and David D. Christ and Michael J. Derelanko and Steve Kutz and Patrick J. Little and Robert N Dehaven and Diane L Dehaven-Hudkins and Roland E. Dolle},
  journal={Journal of medicinal chemistry},
  year={2008},
  volume={51 19},
  pages={
          5893-6
        }
}
Selective delta opioid receptor agonists are promising potential therapeutic agents for the treatment of various types of pain conditions. A spirocyclic derivative was identified as a promising hit through screening. Subsequent lead optimization identified compound 20 (ADL5859) as a potent, selective, and orally bioavailable delta agonist. Compound 20 was selected as a clinical candidate for the treatment of pain. 
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