[2', 6'-Dimethyltyrosine] Dynorphin A (1-11)-NH2 Analogues Lacking an N-Terminal Amino Group: Potent and Selective κ Opioid Antagonists

…, G Weltrowska, I Berezowska, C Lemieux…

Index: Lu; Nguyen; Weltrowska; Berezowska; Lemieux; Chung; Schiller Journal of Medicinal Chemistry, 2001 , vol. 44, # 19 p. 3048 - 3053

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Citation Number: 64

Abstract

Recent studies showed that dermorphin and enkephalin analogues containing two methyl groups at the 2', 6'-positions of the Tyr 1 aromatic ring and lacking an N-terminal amino group were moderately potent δ and μ opioid antagonists. These results indicate that a positively charged N-terminal amino group may be essential for signal transduction but not for receptor binding and suggested that its deletion in agonist opioid peptides containing ...