Abstract
The structure-activity relationships for the 'B-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues have been investigated as TRPV1 receptor antagonists. A docking model of potent antagonist 2 with the sensor region of TRPV1 is proposed.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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CHO Cells
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Cricetinae
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Ligands
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Models, Molecular
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Protein Structure, Tertiary
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Structure-Activity Relationship
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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 / chemistry
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TRPV Cation Channels / metabolism
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Thiocarbamates / chemical synthesis
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Thiocarbamates / chemistry
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Thiourea / analogs & derivatives*
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Thiourea / chemistry
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Thiourea / pharmacology*
Substances
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Ligands
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N-(4-t-butylbenzyl)-N'-(4-(methylsulfonylamino)benzyl)thiourea
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Sulfonamides
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TRPV Cation Channels
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TRPV1 receptor
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Thiocarbamates
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Thiourea