Synthesis and Characterization of Potent and Selective μ-Opioid Receptor Antagonists,[Dmt 1, d-2-Nal4] endomorphin-1 (Antanal-1) and [Dmt1, d-2-Nal4] …

…, NN Chung, C Lemieux, PW Schiller…

Index: Lu, Yixin; Lum, Tze Keong; Augustine, Yoon Wui Leow; Weltrowska, Grazyna; Nguyen, Thi M.-D.; Lemieux, Carole; Chung, Nga N.; Schiller, Peter W. Journal of Medicinal Chemistry, 2006 , vol. 49, # 17 p. 5382 - 5385

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Citation Number: 43

Abstract

To synthesize potent antagonists of the μ-opioid receptor, we prepared a series of endomorphin-1 and endomorphin-2 analogues with 3-(1-naphthyl)-d-alanine (d-1-Nal) or 3- (2-naphthyl)-d-alanine (d-2-Nal) in position 4. Some of these analogues displayed weak