Development of Potent mu and delta Opioid Agonists with High Lipophilicity

作者：Lee Yeon Sun; Kulkarani Vinod; Cowell Scott M; Ma Shou wu; Davis Peg; Hanlon Katherine E; Vanderah Todd W; Lai Josephine; Porreca Flank; Vardanyan Ruben; Hruby Victor J^*

来源：Journal of Medicinal Chemistry, 2011, 54(1): 382-386.

DOI：10.1021/jm100982d

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 mu and delta 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

• 出版日期2011-1-13