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2009.12.14 TRPM8 antagonist(RQ-00203078)が"Thomson Pharma"のIDdb Meeting Reportで紹介されました

TRPM8 antagonist(RQ-00203078)が
"Thomson Pharma"のIDdb Meeting Reportで紹介されました

Neuroscience 2009で発表を行ったラクオリア創薬の新規TRPM8 antagonist(RQ-00203078)が、トムソンロイター社が提供する"Thomson Pharma"にて紹介されました。(以下、IDdb Meeting Report 2009, Oct. 17-21より転載)

A new selective TRPM8 antagonist
Shuzo Watanabe of RaQualia Pharma presented a poster on RQ-00203078, a new selective TRPM8 antagonist in preclinical development for the potential treatment of cold allodynia in patients with neuropathic pain. Previous studies have shown that TRPM8-deficient mice do not display temperature discrimination or hypersensitivity to cold following nerve injury or inflammation, suggesting that TRPM8 is a useful target for cold allodynia. In preclinical rat studies, RQ-00203078 was shown to significantly attenuate cold allodynia at subcutaneous doses of 10 mg/kg and reduce chronic-constriction injury-induced static allodynia. The compound also demonstrated a superior safety profile over pregabalin. At doses up to 100 mg/kg, RQ-00203078 displayed no significant effect on beam walking, a motor performance indicator. In in vitro studies, it showed potent antagonistic activity against human TRPM8.
ポスター: 新規TRPM8 antagonist(RQ-00203078)(PDFファイル:610KB)