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Bioorg Med Chem Lett. 2010 Mar 1;20(5):1610-3. doi: 10.1016/j.bmcl.2010.01.055. Epub 2010 Jan 20.

Novel multiple opioid ligands based on 4-aminobenzazepinone (Aba), azepinoindole (Aia) and tetrahydroisoquinoline (Tic) scaffolds.

Author information

1
Department of Organic Chemistry, Vrije Universiteit Brussel, B-1050 Brussels, Belgium. sballet@vub.ac.be

Abstract

The dimerization and trimerization of the Dmt-Tic, Dmt-Aia and Dmt-Aba pharmacophores provided multiple ligands which were evaluated in vitro for opioid receptor binding and functional activity. Whereas the Tic- and Aba multimers proved to be dual and balanced delta/mu antagonists, as determined by the functional [S(35)]GTPgammaS binding assay, the dimerization of potent Aia-based 'parent' ligands unexpectedly resulted in substantial less efficient receptor binding and non-active dimeric compounds.

PMID:
20137938
PMCID:
PMC2840614
DOI:
10.1016/j.bmcl.2010.01.055
[Indexed for MEDLINE]
Free PMC Article

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