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Development of potent μ and δ opioid agonists with high lipophilicity

Journal of Medicinal Chemistry, ISSN: 0022-2623, Vol: 54, Issue: 1, Page: 382-386
2011
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Article Description

An SAR study on the Dmt-substituted enkephalin-like tetrapeptide with a N-phenyl-N-piperidin-4-ylpropionamide moiety at the C-terminal was performed and has resulted in highly potent ligands at μ and δ opioid receptors. In general, ligands with the substitution of d-Nle and halogenation of the aromatic ring of Phe showed highly increased opioid activities. Ligand 6 with good biological activities in vitro demonstrated potent in vivo antihyperalgesic and antiallodynic effects in the tail-flick assay. © 2010 American Chemical Society.

Bibliographic Details

Lee, Yeon Sun; Kulkarani, Vinod; Cowell, Scott M; Ma, Shou-wu; Davis, Peg; Hanlon, Katherine E; Vanderah, Todd W; Lai, Josephine; Porreca, Frank; Vardanyan, Ruben; Hruby, Victor J

American Chemical Society (ACS)

Biochemistry, Genetics and Molecular Biology; Pharmacology, Toxicology and Pharmaceutics

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