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. The synt...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1998-10, Vol.8 (19), p.2685-2688
Hauptverfasser:	Wang, Chenguang, McFadyen, Iain J., Traynor, John R., Mosberg, Henry I.
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Drug Design Kinetics Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Opioid Peptides - chemical synthesis Opioid Peptides - metabolism Opioid Peptides - pharmacology Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Protein Conformation Receptors, Opioid, delta - agonists Receptors, Opioid, delta - metabolism Receptors, Opioid, mu - agonists Receptors, Opioid, mu - metabolism Stereoisomerism Structure-Activity Relationship
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Zusammenfassung:	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. The synthesis of the potent opioid agonist 7 is described.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(98)00472-7