Ohmi, Masashi published the artcileIdentification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist, Safety of 2-Chloro-3-fluoro-5-(trifluoromethyl)pyridine, the main research area is pyridylbenzensulfonamide derivative RQ00203078 preparation TRPM8 antagonist cold allodynia; structure activity TRPM8 antagonist pyridylbenzensulfonamide derivative RQ00203078; Cold allodynia; RQ-00203078; Sulfonamide; TRPM8 antagonist; Wet-dog shakes.
A novel series of 2-pyridyl-benzensulfonamide derivatives have been identified as selective and orally active TRPM8 antagonists via high throughput screening (HTS). Exploration of the structure-activity relationships of compound (I) has led to the identification of RQ-00203078 (compound 36) as a highly selective, potent and orally available TRPM8 antagonist. RQ-00203078 demonstrated excellent in vivo activity in a dose dependent manner with an ED50 value of 0.65 mg/kg in the icilin-induced wet-dog shakes model in rats after oral administration and may become an important pharmacol. tool for fully assessing the potential therapeutic use of the targets activated by cold stimulation.
Bioorganic & Medicinal Chemistry Letters published new progress about Allodynia (cold). 72600-67-0 belongs to class pyridine-derivatives, name is 2-Chloro-3-fluoro-5-(trifluoromethyl)pyridine, and the molecular formula is C6H2ClF4N, Safety of 2-Chloro-3-fluoro-5-(trifluoromethyl)pyridine.