|
rdf:type |
|
|
lifeskim:mentions |
umls-concept:C0034693,
umls-concept:C0038477,
umls-concept:C0205549,
umls-concept:C0220781,
umls-concept:C0332157,
umls-concept:C0667286,
umls-concept:C0927232,
umls-concept:C1446409,
umls-concept:C1527148,
umls-concept:C1709060,
umls-concept:C1880355,
umls-concept:C1883254
|
|
pubmed:issue |
4
|
|
pubmed:dateCreated |
2011-2-17
|
|
pubmed:abstractText |
Herein we report the discovery, synthesis, and evaluation of a series of N-(4-acetamido)-phenylpicolinamides as positive allosteric modulators of mGlu(4). Compounds from the series show submicromolar potency at both human and rat mGlu(4). In addition, pharmacokinetic studies utilizing subcutaneous dosing demonstrated good brain exposure in rats.
|
|
pubmed:grant |
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Feb
|
|
pubmed:issn |
1520-4804
|
|
pubmed:author |
pubmed-author:BlobaumAnna LAL,
pubmed-author:BolingerJulie DJD,
pubmed-author:ConnP JeffreyPJ,
pubmed-author:EngersDarren WDW,
pubmed-author:FieldJulie RJR,
pubmed-author:HopkinsCorey RCR,
pubmed-author:JadhavSatyawanS,
pubmed-author:JonesCarrie KCK,
pubmed-author:LeUyenU,
pubmed-author:LindsleyCraig WCW,
pubmed-author:NiswenderColleen MCM,
pubmed-author:WeaverC DavidCD,
pubmed-author:ZamoranoRocioR,
pubmed-author:ZhouYaY
|
|
pubmed:issnType |
Electronic
|
|
pubmed:day |
24
|
|
pubmed:volume |
54
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
1106-10
|
|
pubmed:dateRevised |
2011-9-13
|
|
pubmed:meshHeading |
pubmed-meshheading:21247167-Allosteric Regulation,
pubmed-meshheading:21247167-Animals,
pubmed-meshheading:21247167-Brain,
pubmed-meshheading:21247167-CHO Cells,
pubmed-meshheading:21247167-Central Nervous System,
pubmed-meshheading:21247167-Cricetinae,
pubmed-meshheading:21247167-Cricetulus,
pubmed-meshheading:21247167-Humans,
pubmed-meshheading:21247167-Magnetic Resonance Spectroscopy,
pubmed-meshheading:21247167-Mass Spectrometry,
pubmed-meshheading:21247167-Picolines,
pubmed-meshheading:21247167-Rats,
pubmed-meshheading:21247167-Receptors, Metabotropic Glutamate,
pubmed-meshheading:21247167-Structure-Activity Relationship
|
|
pubmed:year |
2011
|
|
pubmed:articleTitle |
Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats.
|
|
pubmed:affiliation |
Department of Pharmacology, Vanderbilt University Medical Center, Nashville, Tennessee 37232, United States.
|
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't,
Research Support, N.I.H., Extramural
|
