Novel 3,4,7-Substituted Benzofuran Derivatives Having Binding Affinity to κ-Opioid Receptor

Daisuke Nishiyama; Yuki Sakai; Haruka Sekiguchi; Hiroaki Chiba; Ryosuke Misu; Shinya Oishi; Nobutaka Fujii; Hiroaki Ohno

doi:10.1248/cpb.c16-00302

Special Collection of Papers: Notes

Novel 3,4,7-Substituted Benzofuran Derivatives Having Binding Affinity to κ-Opioid Receptor

Daisuke Nishiyama, Yuki Sakai, Haruka Sekiguchi, Hiroaki Chiba, Ryosuke Misu, Shinya Oishi, Nobutaka Fujii, Hiroaki Ohno

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Keywords: κ-opioid receptor, opioid, benzofuran, morphine

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2016 Volume 64 Issue 7 Pages 996-1003

DOI https://doi.org/10.1248/cpb.c16-00302

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Abstract

A series of novel 3,4,7-trisubstituted benzofuran derivatives were synthesized, and their binding affinity to κ- (KOR) and μ-opioid receptors (MOR) were evaluated. Several aryl ethers showed moderate binding activities to KOR (IC₅₀=3.9–11 µM) without binding to MOR.

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