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

Article Details

Citation

Wang C, McFadyen IJ, Traynor JR, Mosberg HI

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

Bioorg Med Chem Lett. 1998 Oct 6;8(19):2685-8.

PubMed ID
9873603 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
FentanylKappa-type opioid receptorKi (nM)1130N/AN/ADetails
FentanylMu-type opioid receptorKi (nM)8.45N/AN/ADetails
MorphineKappa-type opioid receptorKi (nM)110N/AN/ADetails
MorphineMu-type opioid receptorKi (nM)6.51N/AN/ADetails