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. 2014 Dec 1;24(23):5364-8.
doi: 10.1016/j.bmcl.2014.10.074. Epub 2014 Oct 29.

Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist

Masashi Ohmi  1 , Yuji Shishido  2 , Tadashi Inoue  2 , Kazuo Ando  2 , Akiyoshi Fujiuchi  2 , Akiko Yamada  2 , Shuzo Watanabe  2 , Kiyoshi Kawamura  3
Affiliations

Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist

Masashi Ohmi et al. Bioorg Med Chem Lett. .

Abstract

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.

Keywords: Cold allodynia; RQ-00203078; Sulfonamide; TRPM8 antagonist; Wet-dog shakes.

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