rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
16
|
pubmed:dateCreated |
2010-8-9
|
pubmed:abstractText |
As part of the vital search towards improved therapeutic agents for the treatment of neuropathic pain, the central nervous system glutamate receptors have become a major focus of research. Outlined herein are the syntheses of two new biologically active 3'-cycloalkyl-substituted carboxycyclopropylglycines, utilizing novel synthetic chemistry. The reaction between substituted 1,2-dioxines and an aminophosphonate furnished the cyclopropane core in a single step with all required stereochemistry of pendant groups. In vitro binding assays at metabotropic glutamate receptors revealed selective activity. In vivo testing in a rodent model of neuropathic pain indicated one amino acid significantly and dose-dependently decreased mechanical allodynia.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Aug
|
pubmed:issn |
1464-3391
|
pubmed:author |
pubmed-author:AbellAndrew DAD,
pubmed-author:AveryThomas DTD,
pubmed-author:Bräuner-OsborneHansH,
pubmed-author:HutchinsonMark RMR,
pubmed-author:IrvineRodney JRJ,
pubmed-author:KvistTrineT,
pubmed-author:MathiesenJesper MosolffJM,
pubmed-author:NielsenBirgitteB,
pubmed-author:PedersenDaniel SejerDS,
pubmed-author:StanleyNathan JNJ,
pubmed-author:TaylorDennis KDK,
pubmed-author:TiekinkEdward R TER
|
pubmed:copyrightInfo |
Copyright 2010 Elsevier Ltd. All rights reserved.
|
pubmed:issnType |
Electronic
|
pubmed:day |
15
|
pubmed:volume |
18
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
6089-98
|
pubmed:meshHeading |
pubmed-meshheading:20638290-Analgesics,
pubmed-meshheading:20638290-Animals,
pubmed-meshheading:20638290-CHO Cells,
pubmed-meshheading:20638290-Cricetinae,
pubmed-meshheading:20638290-Cricetulus,
pubmed-meshheading:20638290-Cyclopropanes,
pubmed-meshheading:20638290-Glycine,
pubmed-meshheading:20638290-Hyperalgesia,
pubmed-meshheading:20638290-Male,
pubmed-meshheading:20638290-Neuralgia,
pubmed-meshheading:20638290-Rats,
pubmed-meshheading:20638290-Rats, Sprague-Dawley,
pubmed-meshheading:20638290-Receptors, Metabotropic Glutamate
|
pubmed:year |
2010
|
pubmed:articleTitle |
A new metabotropic glutamate receptor agonist with in vivo anti-allodynic activity.
|
pubmed:affiliation |
Discipline of Chemistry, The University of Adelaide, Adelaide, Australia.
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|