|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
3
|
|
pubmed:dateCreated |
2005-1-24
|
|
pubmed:abstractText |
Seventeen biarylcarboxybenzamide derivatives were prepared for the study of their agonistic/antagonistic activities to the vanilloid receptor (VR1) in rat DRG neurons. The replacement of the piperazine moiety of the lead compound 1 with phenyl ring showed quite enhanced antagonistic activity. Among the prepared derivatives, N-(4-tert-butylphenyl)-4-pyridine-2-yl-benzamide (2, IC(50)=31 nM) and N-(4-tert-butylphenyl)-4-(3-methylpyridine-2-yl)benzamide (3g, IC(50)=31 nM), showed 5-fold higher antagonistic activity than 1 in (45)Ca(2+)-influx assay.
|
|
pubmed:commentsCorrections |
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Feb
|
|
pubmed:issn |
0960-894X
|
|
pubmed:author |
pubmed-author:ChoHawonH,
pubmed-author:ChoiJi-YeonJY,
pubmed-author:ChoiSea-HoonSH,
pubmed-author:JeongYeon SuYS,
pubmed-author:JewSang-SupSS,
pubmed-author:JooYung HyupYH,
pubmed-author:KimHee-DooHD,
pubmed-author:KimJin KwanJK,
pubmed-author:KimMi-HyunMH,
pubmed-author:KohHyun-JuHJ,
pubmed-author:LeeJihyeJ,
pubmed-author:OhUhtaekU,
pubmed-author:ParkHyeung-GeunHG,
pubmed-author:ParkMi-KyungMK,
pubmed-author:ParkYoung-HoYH,
pubmed-author:ShinSong SeokSS,
pubmed-author:SuhYoung-GerYG
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
1
|
|
pubmed:volume |
15
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
631-4
|
|
pubmed:dateRevised |
2006-11-15
|
|
pubmed:meshHeading |
pubmed-meshheading:15664827-Animals,
pubmed-meshheading:15664827-Benzamides,
pubmed-meshheading:15664827-Calcium Signaling,
pubmed-meshheading:15664827-Ganglia, Spinal,
pubmed-meshheading:15664827-Inhibitory Concentration 50,
pubmed-meshheading:15664827-Ion Channels,
pubmed-meshheading:15664827-Ligands,
pubmed-meshheading:15664827-Neurons,
pubmed-meshheading:15664827-Rats,
pubmed-meshheading:15664827-Receptors, Drug,
pubmed-meshheading:15664827-Structure-Activity Relationship,
pubmed-meshheading:15664827-TRPV Cation Channels
|
|
pubmed:year |
2005
|
|
pubmed:articleTitle |
Biarylcarboxybenzamide derivatives as potent vanilloid receptor (VR1) antagonistic ligands.
|
|
pubmed:affiliation |
Research Institute of Pharmaceutical Sciences and College of Pharmacy, Seoul National University, Seoul 151-742, South Korea. hgpk@plaza.snu.ac.kr
|
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|
