| Literature DB >> 19892550 |
Shijun Zhang1, Ajay Yekkirala, Ye Tang, Philip S Portoghese.
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.Entities:
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Year: 2009 PMID： 19892550 PMCID： PMC5060004 DOI： 10.1016/j.bmcl.2009.10.045
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823