2. Academic Validation
  3. Development of potent μ and δ opioid agonists with high lipophilicity

Development of potent μ and δ opioid agonists with high lipophilicity

  • J Med Chem. 2011 Jan 13;54(1):382-6. doi: 10.1021/jm100982d.
Yeon Sun Lee 1,  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
Affiliations

Affiliation

  • 1 Department of Chemistry and Biochemistry, University of Arizona, Tucson, Arizona 85721, United States.
PMID: 21128594 DOI: 10.1021/jm100982d
Abstract

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.

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