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Design, synthesis, and pharmacological evaluation of phenoxy pyridyl derivatives as dual norepinephrine reuptake inhibitors and 5-HT1A partial agonists.

Abstract：

:Preclinical studies suggest that compounds with dual norepinephrine reuptake inhibitor (NRI) and 5-HT(1A) partial agonist properties may provide an important new therapeutic approach to ADHD, depression, and anxiety. Reported herein is the discovery of a novel chemical series with a favorable NRI and 5-HT(1A) partial agonist pharmacological profile as well as excellent selectivity for the norepinephrine transporter over the dopamine transporter.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Dounay AB,Barta NS,Campbell BM,Coleman C,Collantes EM,Denny L,Dutta S,Gray DL,Hou D,Iyer R,Maiti SN,Ortwine DF,Probert A,Stratman NC,Subedi R,Whisman T,Xu W,Zoski K

doi

10.1016/j.bmcl.2009.12.023

subject

Has Abstract

pub_date

2010-02-01 00:00:00

pages

1114-7

issue

3

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(09)01728-4

journal_volume

20

pub_type

杂志文章

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