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Novel C-terminus modifications of the Dmt-Tic motif: a new class of dipeptide analogues showing altered pharmacological profiles toward the opioid receptors.

Abstract：

:The design, synthesis and pharmacological evaluation of a novel class of Dmt-Tic dipeptide analogues are described. These resulting analogues bearing different C-terminal functionalities were found to bind to the human delta receptor with high affinity. One specific class of dipeptides bearing urea/thiourea functionalities showed partial to full activation of the delta receptor. Several dipeptides also showed good binding affinities with full activation of the human kappa receptor, a novel property for those ligands.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Pagé D,Naismith A,Schmidt R,Coupal M,Labarre M,Gosselin M,Bellemare D,Payza K,Brown W

doi

10.1021/jm015532k

keywords:

subject

Has Abstract

pub_date

2001-07-19 00:00:00

pages

2387-90

issue

15

eissn

0022-2623

issn

1520-4804

pii

jm015532k

journal_volume

44

pub_type

杂志文章

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