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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

DOI: 10.1016/j.bmcl.2009.10.045