1254207-33-4Relevant articles and documents
Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist
Ohmi, Masashi,Shishido, Yuji,Inoue, Tadashi,Ando, Kazuo,Fujiuchi, Akiyoshi,Yamada, Akiko,Watanabe, Shuzo,Kawamura, Kiyoshi
, p. 5364 - 5368 (2015/01/08)
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 1 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 pharmacological tool for fully assessing the potential therapeutic use of the targets activated by cold stimulation.
