Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist was written by Ohmi, Masashi;Shishido, Yuji;Inoue, Tadashi;Ando, Kazuo;Fujiuchi, Akiyoshi;Yamada, Akiko;Watanabe, Shuzo;Kawamura, Kiyoshi. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2014.Recommanded Product: 3-Fluoro-5-(trifluoromethyl)pyridin-2-amine This article mentions the following:
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. In the experiment, the researchers used many compounds, for example, 3-Fluoro-5-(trifluoromethyl)pyridin-2-amine (cas: 852062-17-0Recommanded Product: 3-Fluoro-5-(trifluoromethyl)pyridin-2-amine).
3-Fluoro-5-(trifluoromethyl)pyridin-2-amine (cas: 852062-17-0) belongs to pyridine derivatives. The ring atoms in the pyridine molecule are sp2-hybridized. The nitrogen is involved in the π-bonding aromatic system using its unhybridized p orbital. The lone pair is in an sp2 orbital, projecting outward from the ring in the same plane as the σ bonds. Several pyridine derivatives play important roles in biological systems. While its biosynthesis is not fully understood, nicotinic acid (vitamin B3) occurs in some bacteria, fungi, and mammals.Recommanded Product: 3-Fluoro-5-(trifluoromethyl)pyridin-2-amine