Synthesis and evaluation of thiazole carboxamides as vanilloid receptor 1 (TRPV1) antagonists.

TL;DR: The in vitro and in vivo characterization of a novel and selective TRPV1 antagonist, AMG 517, and its pharmacology with that of a closely related analog, tert-butyl-2-(6-([2-(acetylamino)-1,3-benzothiazol-4-yl]oxy)pyrimidin- 4-yl)-5-(trifluoromethyl)phenylcarbamate (AMG8163) suggest that

TL;DR: Based on a series of diaryl amides the corresponding inverse amides have been found to be potent TRPV1 receptor antagonists and indazolone 4a was identified as a novel TRPv1 receptor antagonist suitable for evaluating orally in animal models of analgesia.

TL;DR: This review is to provide an overview of synthesized compounds possessing perfluoroalkylated or polyfluorinated chains that have been tested for bioactivity or as potential drug candidates for the treatment of various diseases.

TL;DR: A review of the patent literature related to non-peptidic small molecule TRPV1 antagonists finds interest in this approach toward the treatment of various pain conditions appears to be growing annually.

TL;DR: AMG 9810 is the first cinnamide TRPV1 antagonist reported to block capsaicin-induced eye wiping behavior and reverse hyperalgesia in an animal model of inflammatory pain.

TL;DR: The molecular, pharmacological and physiological characteristics, and putative functions, of the vanilloid receptor 1 are summarized, and the therapeutic potential of this molecule is discussed.