Synthesis of quinolinomorphinan derivatives as highly selective δ opioid receptor ligands

…, A Matsubara, T Nemoto, M Saito, S Hirayama…

Index: Ida, Yoshihiro; Matsubara, Ayaka; Nemoto, Toru; Saito, Manabu; Hirayama, Shigeto; Fujii, Hideaki; Nagase, Hiroshi Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 19 p. 5810 - 5831

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Citation Number: 10

Abstract

We have reported previously the novel δ opioid agonist KNT-127 which showed high affinity and selectivity for the δ receptor. Moreover, the analgesic effect of subcutaneously administered KNT-127 was more potent than that of a prototypical δ agonist (−)-TAN-67 in the acetic acid writhing test. This study of the structure–activity relationship of KNT-127 derivatives focused on the introduction of substituents onto the 5′-, 6′-, 7′-or 8′- ...