Systemic analgesic activity and .delta.-opioid selectivity in [2,6-dimethyl-Tyr1, D-Pen2, D-Pen5]enkephalin

The cyclic peptide [2,6-dimethyl-Tyr1,D-Pen2,D-Pen5]enkephalin (2) was synthesized by solid-phase techniques and contains the optically pure unnatural amino acid 2,6-dimethyltyrosine (DMT) as a replacement for the Tyr1 residue of [D-Pen2,D-Pen5]enkephalin (DPDPE, 1). This structural modification res...

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Veröffentlicht in:	Journal of medicinal chemistry 1992-02, Vol.35 (4), p.684-687
Hauptverfasser:	Hansen, Donald W, Stapelfeld, Awilda, Savage, Michael A, Reichman, Melvin, Hammond, Donna L, Haaseth, Ronald C, Mosberg, Henry I
Format:	Artikel
Sprache:	eng
Schlagworte:	Analgesia Analgesics - chemical synthesis Analgesics - metabolism Analgesics - pharmacology Animals Brain - metabolism Cell Membrane - metabolism Chemistry Electric Stimulation Enkephalins - chemical synthesis Enkephalins - metabolism Enkephalins - pharmacology Exact sciences and technology Male Mice Mice, Inbred ICR Muscle Contraction - drug effects Organic chemistry Pain Measurement Peptides Preparations and properties Receptors, Opioid - physiology Receptors, Opioid, delta Receptors, Opioid, mu Structure-Activity Relationship Vas Deferens - drug effects Vas Deferens - physiology
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