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ID: ALA1156740
Journal: Bioorg Med Chem Lett
Title: A bivalent ligand (KMN-21) antagonist for mu/kappa heterodimeric opioid receptors.
Authors: Zhang S, Yekkirala A, Tang Y, Portoghese PS.
Abstract: In an effort to develop antagonists for kappa-mu opioid receptor heterodimers, a series of bivalent ligands 3-6 containing kappa- and mu-antagonist pharmacophores were designed and synthesized. Evaluation of the series in HEK-293 cells revealed 4 (KMN-21) to selectively antagonize the activation of kappa-mu heterodimers, suggesting possible bridging of receptors when the bivalent ligand spacer contains 21 atoms.
CiteXplore: 19892550