Design, Synthesis, and Evaluation of Opioid Analogues with Non-Peptidic β-Turn Scaffold:  Enkephalin and Endomorphin Mimetics

Design, Synthesis, and Evaluation of Opioid Analogues with Non-Peptidic β-Turn Scaffold:  Enkephalin and Endomorphin Mimetics Endomorphin-2 with a β-Turn Backbone Constraint Retains the Potent μ-Opioid Receptor Agonist Properties Endomorphin-1 Analogues Containing β-Proline Are μ-Opioid Receptor Agonists and Display Enhanced Enzymatic Hydrolysis Resistance Synthesis and binding activity of endomorphin-1 analogues containing β-amino acids Design of a high affinity peptidomimetic opioid agonist from peptide pharmacophore models Endomorphin analogues with mixed μ-opioid (MOP) receptor agonism/δ-opioid (DOP) receptor antagonism and lacking β-arrestin2 recruitment activity Constraining Endomorphin-1 by β,α-Hybrid Dipeptide/Heterocycle Scaffolds: Identification of a Novel κ-Opioid Receptor Selective Partial Agonist Synthesis and Evaluation of the Affinity toward μ-Opioid Receptors of Atypical, Lipophilic Ligands Based on the Sequencec[-Tyr-Pro-Trp-Phe-Gly-] Design, Synthesis, Pharmacological Evaluation, and Structure−Activity Study of Novel Endomorphin Analogues with Multiple Structural Modifications New Endomorphin Analogues Containing Alicyclic β-Amino Acids: Influence on Bioactive Conformation and Pharmacological Profile