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CCK1-antagonists: Design, Synthesis and Evaluation of N-Substituted Isobuyl-5-Hydroxy-5-Phenyl-Pyrrol-2-Ones as Adjunct to Opiates

Author

Listed:
  • Eric Lattmann

    (School of Life and Health Sciences, Aston University, England)

  • Jintana Sattayasai

    (Department of Pharmacology, Faculty of Medicine, Khon Kaen University, Thailand)

  • Ramesh Narayanan

    (Department of Medicine, University of Tennessee Health Science Center, USA)

  • Julian Benyamen
  • PN Balaram
  • Pornthip Lattmann

    (PNB Vesper Life Science PVT, India)

Abstract

Arylated 5-hydroxy–pyrrol-2-ones were prepared in 2 synthetic steps from muco- chloric acid and were optimised as CCK selective ligands using radiolabelled binding assays. A potent CCK1 selective ligand was identified ( PNB-081: CCK1= 20 nM) as part of systematic SAR optimisation. The antagonism was confirmed for the ligands by using isolated tissue preparations with CCK8S. The cholecystokinin antagonist PNB-081 potentiated the analgesic effect of morphine and reversed opiate tolerance in mice from doses >1 mg/kg by oral administration.

Suggested Citation

  • Eric Lattmann & Jintana Sattayasai & Ramesh Narayanan & Julian Benyamen & PN Balaram & Pornthip Lattmann, 2018. "CCK1-antagonists: Design, Synthesis and Evaluation of N-Substituted Isobuyl-5-Hydroxy-5-Phenyl-Pyrrol-2-Ones as Adjunct to Opiates," Organic & Medicinal Chemistry International Journal, Juniper Publishers Inc., vol. 5(5), pages 138-147, March.
    • Handle: RePEc:adp:jomcij:v:5:y:2018:i:5:p:138-147
    DOI: 10.19080/OMCIJ.2018.05.555672
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