Abstract
We have developed a new class of diarylalkyl amides as novel TRPV1 antagonists. They exhibited potent (45)Ca(2+) uptake inhibitions in rat DRG neuron. In particular, the amide 59 was identified as a potent antagonist with IC(50) of 57 nM. The synthesis and structure-activity relationship of the diarylalkyl amides are also described.
MeSH terms
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Amides / chemical synthesis*
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Amides / chemistry
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Amides / pharmacology
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Animals
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Calcium / metabolism
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Cells, Cultured
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Drug Design
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Inhibitory Concentration 50
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Rats
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Rats, Sprague-Dawley
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis*
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Sulfonamides / chemistry
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Sulfonamides / pharmacology
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TRPV Cation Channels / antagonists & inhibitors*
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TRPV Cation Channels / metabolism
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Tetrahydronaphthalenes / chemical synthesis*
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Tetrahydronaphthalenes / chemistry
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Tetrahydronaphthalenes / pharmacology
Substances
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Amides
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N-(3-cyano-5-fluoro-4-(methylsulfonamido)benzyl)-3-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)propanamide
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Sulfonamides
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TRPV Cation Channels
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Tetrahydronaphthalenes
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Trpv1 protein, rat
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Calcium