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Tetrahydroquinoline derivatives as opioid receptor antagonists.

Abstract：

:Opioid receptors play an important role in both behavioral and homeostatic functions. We herein report tetrahydroquinoline derivatives as opioid receptor antagonists. SAR studies led to the identification of the potent antagonist 2v, endowed with 1.58nM (K(i)) functional activity against the μ opioid receptor. DMPK data suggest that novel tetrahydroquinoline analogs may be advantageous in peripheral applications.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Zhang C,Westaway SM,Speake JD,Bishop MJ,Goetz AS,Carballo LH,Hu M,Epperly AH

doi

10.1016/j.bmcl.2010.12.010

subject

Has Abstract

pub_date

2011-01-15 00:00:00

pages

670-6

issue

2

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)01764-6

journal_volume

21

pub_type

杂志文章

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