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Design of a high affinity peptidomimetic opioid agonist from peptide pharmacophore models
C Wang1, I J McFadyen, J R Traynor
1College of Pharmacy, University of Michigan, Ann Arbor 48109, USA.
Bioorganic & Medicinal Chemistry Letters
|January 5, 1999
Abstract:
A pair of diastereomeric peptidomimetics based upon opioid receptor-binding pharmacophore models derived for a series of opioid tetrapeptides was synthesized. Both analogues display high opioid receptor affinity, moderate selectivity for the mu opioid receptor, and are potent, full agonists.