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Lee YS Kulkarani V Cowell SM Ma SW Davis P Hanlon KE Vanderah TW Lai J Porreca F Vardanyan R Hruby VJ 《Journal of medicinal chemistry》2011,54(1):382-386
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(2) and halogenation of the aromatic ring of Phe(4) 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. 相似文献
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