Article
A novel RyR1-selective inhibitor prevents and rescues sudden death in mouse models of malignant hyperthermia and heat stroke.
Nature communications - 13 Jul 2021
Yamazawa Toshiko, Kobayashi Takuya, Kurebayashi Nagomi, Konishi Masato, Noguchi Satoru, Inoue Takayoshi, Inoue Yukiko U, Nishino Ichizo, Mori Shuichi, Iinuma Hiroto, Manaka Noriaki, Kagechika Hiroyuki, Uryash Arkady, Adams Jose, Lopez Jose R, Liu Xiaochen, Diggle Christine, Allen Paul D, Kakizawa Sho, Ikeda Keigo, Lin Bangzhong, Ikemi Yui, Nunomura Kazuto, Nakagawa Shinsaku, Sakurai Takashi, Murayama Takashi
Abstract excerpt
Mutations in the type 1 ryanodine receptor (RyR1), a Ca2+ release channel in skeletal muscle, hyperactivate the channel to cause malignant hyperthermia (MH) and are implicated in severe heat stroke. Dantrolene, the only approved drug for MH, has the disadvantages of having very poor water solubility and long plasma half-life. We show here that an oxolinic acid-derivative RyR1-selective inhibitor,...
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