A potent and selective cis-amide inhibitor of ryanodine receptor 2 as a candidate for cardiac arrhythmia treatment

• Published in: European journal of medicinal chemistry Vol. 262; p. 115910
• Main Authors: Ishida, Ryosuke, Kurebayashi, Nagomi, Iinuma, Hiroto, Zeng, Xi, Mori, Shuichi, Kodama, Masami, Murayama, Takashi, Masuno, Hiroyuki, Takeda, Fumi, Kawahata, Masatoshi, Tanatani, Aya, Miura, Aya, Nishio, Hajime, Sakurai, Takashi, Kagechika, Hiroyuki
• Format: Journal Article
• Language: English
• Published: ISSY-LES-MOULINEAUX Elsevier Masson SAS 15.12.2023; Elsevier
• Subjects: Arrhythmias drug candidate; Ca2+ channel inhibitor; Chemistry, Medicinal; Life Sciences & Biomedicine; Pharmacology & Pharmacy; Ryanodine receptor 2; Science & Technology; Structure-activity relationship; Arrhythmias drug candidate; Ryanodine receptor 2; Ca2+ channel inhibitor; Structure-activity relationship; POLYMORPHIC VENTRICULAR-TACHYCARDIA; TETRAZOLES; DANTROLENE; MALIGNANT HYPERTHERMIA; CONVERSION; SARCOPLASMIC-RETICULUM; RELEASE CHANNEL; PHARMACOLOGY; Ca 2+channel inhibitor; MOUSE MODEL; MUTATIONS

Ryanodine receptor 2 (RyR2) is a Ca2+ release channel mainly located on the sarcoplasmic reticulum (SR) membrane of heart muscle cells and regulates the concentration of Ca2+ in the cytosol. RyR2 overactivation causes potentially lethal cardiac arrhythmias, but no specific inhibitor is yet available...