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rdf:type |
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lifeskim:mentions |
umls-concept:C0079883,
umls-concept:C0205177,
umls-concept:C0205314,
umls-concept:C0205531,
umls-concept:C0226896,
umls-concept:C0243072,
umls-concept:C0243076,
umls-concept:C0392756,
umls-concept:C0442027,
umls-concept:C0599260,
umls-concept:C0679622,
umls-concept:C1167622,
umls-concept:C1416572,
umls-concept:C1510827,
umls-concept:C1527415,
umls-concept:C1880355
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pubmed:issue |
20
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pubmed:dateCreated |
2007-9-18
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pubmed:abstractText |
Novel NR2B antagonists with an amide tether were found by an approach to avoid pharmacophoric similarity to dofetilide. Structure-activity relationship investigation led to N-[cis-4-hydroxy-4-(5-hydroxypyridin-2-yl)cyclohexyl]-3-henylpropanamide as an orally active NR2B-subtype selective N-methyl-D-aspartate (NMDA) receptor antagonist with very weak HERG (human ether-a-go-go related gene) binding (IC(50)> 30 microM). This compound exhibited potent in vivo anti-allodynic activity in the mouse partial sciatic nerve ligation (PSL) model (minimum effective dose=10 mg/kg, po).
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Oct
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:AndoKazuoK,
pubmed-author:HattoriKazunariK,
pubmed-author:KawaiMakotoM,
pubmed-author:KawamuraMitsuhiroM,
pubmed-author:MatsumizuMiyakoM,
pubmed-author:NakamuraHiroshiH,
pubmed-author:NukuiSeijiS,
pubmed-author:OhtaAtsukoA,
pubmed-author:OmuraAtsushiA,
pubmed-author:SakuradaIsaoI,
pubmed-author:ShimokawaHirohisaH,
pubmed-author:TanakaHirotakaH
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pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
17
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5533-6
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pubmed:meshHeading |
pubmed-meshheading:17768047-Administration, Oral,
pubmed-meshheading:17768047-Drug Design,
pubmed-meshheading:17768047-Ether-A-Go-Go Potassium Channels,
pubmed-meshheading:17768047-Inhibitory Concentration 50,
pubmed-meshheading:17768047-Molecular Structure,
pubmed-meshheading:17768047-N-Methylaspartate,
pubmed-meshheading:17768047-Pyridines,
pubmed-meshheading:17768047-Receptors, N-Methyl-D-Aspartate,
pubmed-meshheading:17768047-Solubility,
pubmed-meshheading:17768047-Structure-Activity Relationship
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pubmed:year |
2007
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pubmed:articleTitle |
Discovery of novel and orally active NR2B-selective N-methyl-D-aspartate (NMDA) antagonists, pyridinol derivatives with reduced HERG binding affinity.
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pubmed:affiliation |
Discovery Chemistry, Pfizer Global Research & Development, Nagoya Laboratories, 5-2 Taketoyo, Aichi 470-2393, Japan. makoto.kawai@pfizer.com
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pubmed:publicationType |
Journal Article
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