Document Detail


N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats.
MedLine Citation:
PMID:  23727046     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Development of SAR in an N-acyl-N'-arylpiperazine series of negative allosteric modulators of mGlu1 using a functional cell-based assay is described in this Letter. Characterization of selected compounds in protein binding assays was used to aid in selecting VU0469650 for further profiling in ancillary pharmacology assays and pharmacokinetic studies. VU0469650 demonstrated an excellent selectivity profile and good exposure in both plasma and brain samples following intraperitoneal dosing in rats.
Authors:
Kimberly M Lovell; Andrew S Felts; Alice L Rodriguez; Daryl F Venable; Hyekyung P Cho; Ryan D Morrison; Frank W Byers; J Scott Daniels; Colleen M Niswender; P Jeffrey Conn; Craig W Lindsley; Kyle A Emmitte
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2013-05-17
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  23     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2013 Jul 
Date Detail:
Created Date:  2013-06-10     Completed Date:  2014-01-13     Revised Date:  2014-07-02    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  3713-8     Citation Subset:  IM    
Copyright Information:
Copyright © 2013 Elsevier Ltd. All rights reserved.
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MeSH Terms
Descriptor/Qualifier:
Allosteric Regulation / drug effects*
Animals
Central Nervous System / drug effects*,  metabolism
Dose-Response Relationship, Drug
Molecular Structure
Piperazines / chemical synthesis,  chemistry,  pharmacology*
Rats
Receptors, Metabotropic Glutamate / antagonists & inhibitors*,  metabolism
Structure-Activity Relationship
Grant Support
ID/Acronym/Agency:
U19 MH097056/MH/NIMH NIH HHS
Chemical
Reg. No./Substance:
0/Piperazines; 0/Receptors, Metabotropic Glutamate; 0/VU0469650; 0/metabotropic glutamate receptor type 1
Comments/Corrections

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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