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- W2076249178 abstract "A series of N-[{2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)-pyridin-3-yl}methyl] N′-(6,6-fused heterocyclic) ureas have been investigated as hTRPV1 antagonists. Among them, compound 15 showed highly potent TRPV1 antagonism to capsaicin, with Ki(ant) = 0.2 nM, as well as antagonism to other activators, and it was efficacious in a pain model. A docking study of 15 with our hTRPV1 homology model indicates that there is crucial hydrogen bonding between the ring nitrogen and the receptor, contributing to its potency." @default.
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- W2076249178 date "2015-02-01" @default.
- W2076249178 modified "2023-10-07" @default.
- W2076249178 title "6,6-Fused heterocyclic ureas as highly potent TRPV1 antagonists" @default.
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- W2076249178 doi "https://doi.org/10.1016/j.bmcl.2014.12.086" @default.
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