3-Aryl pyridone derivatives. Potent and selective kappa opioid receptor agonists

…, J Georgsson, M Johansson, M Lindschoten…

Index: Semple, Graeme; Andersson, Britt-Marie; Chhajlani, Vijay; Georgsson, Jennie; Johansson, Magnus; Lindschoten, Marcel; Ponten, Fritof; Rosenquist, Asa; Soerensen, Henrik; Swanson, Lars; Swanson, Marianne Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 2 p. 197 - 200

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Citation Number: 10

Abstract

A new series of 3-aryl pyridone based kappa opioid receptor agonists was designed and synthesised, based on an understanding of the classical kappa opioid receptor pharmacophore. The most potent of the new compounds were comparable to U-69,593 in receptor affinity, selectivity and functional agonist effect at the cloned human kappa opioid receptor.