Novel Dmt-Tic dipeptide analogues as selective delta-opioid receptor antagonists

…, T Mischki, R Schmidt, J Butterworth, S St-Onge…

Index: Page; McClory; Mischki; Schmidt; Butterworth; St-Onge; Labarre; Payza; Brown Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 2 p. 167 - 170

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Citation Number: 21

Abstract

A series of Dmt-Tic analogues with substitution on the Tic aromatic ring has been synthesized and evaluated for opioid receptor affinity and activation. Incorporation of large hydrophobic groups at position 7 of Tic did not greatly alter the δ opioid receptor binding affinities of the dipeptides whereas substitution at position 6 substantially diminished their affinity. These modified Dmt-Tic peptides showed binding affinities as low as 2.5 nM with ...