Development of Potent 渭 and 未 Opioid Agonists with High Lipophilicity

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• 作者：Yeon Sun Lee ; Vinod Kulkarani ; Scott M. Cowell ; Shou-wu Ma ; Peg Davis ; Katherine E. Hanlon ; Todd W. Vanderah ; Josephine Lai ; Frank Porreca ; Ruben Vardanyan ; Victor J. Hruby
• 刊名：Journal of Medicinal Chemistry
• 出版年：2011
• 出版时间：January 13, 2011
• 年：2011
• 卷：54
• 期：1
• 页码：382-386
• 全文大小：740K
• 年卷期：v.54,no.1(January 13, 2011)
• ISSN：1520-4804

文摘

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 渭 and 未 opioid receptors. In general, ligands with the substitution of d-Nle² and halogenation of the aromatic ring of Phe⁴ 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.