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KMID : 0043320090320091201
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Archives of Pharmacal Research
2009 Volume.32 No. 9 p.1201 ~ p.1210
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Design, Synthesis, and Biological Evaluation of Phenylpropanamides as Novel Transient Receptor Potential Valnilloid 1 Antagonists
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Suh Young-Ger
Li Fu-Nan
Kim Nam-Jung
Nam Yeon-Hee
Kim Seung-Hee
Seo Seung-Yong
Jeong Yeon-Su
Kim Sun-Young
Park Young-Ho
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Abstract
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Synthesis and structure-activity relationship of N-benzyl-3-phenylpropanamides as transient receptor potential vanilloid 1 (TRPV1) antagonists are described. A variety of substituents such as halide, ester, nitro, and alkyl groups at 2 or 3-position of 4-(methylsulfonylamino) benzyl unit were examined. These compounds exhibited potent 45Ca2+ uptake inhibition in rat DRG neuron via TRPV1 blockade. Especially compound 28c, has been identified as a potent antagonist with IC50 of 38 nM.
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KEYWORD
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Synthesis, Amide, Analogues, TRPV1, Antagonists
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