Design of a high affinity peptidomimetic opioid agonist from peptide pharmacophore models

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 μ opioid receptor, and are potent, full agonists.