Analogs of the. delta. opioid receptor selective cyclic peptide [cyclic][2-D-penicillamine, 5-D-penicillamine]-enkephalin: 2', 6'-dimethyltyrosine and Gly3-Phe4 amide …

…, MA Savage, LN Williamson, M Reichman

Index: Chandrakumar; Stapelfeld; Beardsley; Lopez; Drury; Anthony; Savage; Williamson; Reichman Journal of Medicinal Chemistry, 1992 , vol. 35, # 16 p. 2928 - 2938

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Citation Number: 30

Abstract

In order to develop systemically-active opioid peptidea, the &selective, opioid pentapeptide [~-Pen*,~-Pen~]-enkephalin (DPDPE) was modified by eaterification and by substitution of 2', 6'-dimethyltyrosine for tyrosine to yield 4. Compound 4 was on the order of 8-and 800-fold more active than DPDPE in both 6 and p opioid radioligand binding assays, respectively, in rat neural membrane suspensions. Compound 4 was considerably more potent than ...