Preclinical characterization of [18F]T-008, a novel PET imaging radioligand for cholesterol 24-hydroxylase

• Published in: European journal of nuclear medicine and molecular imaging Vol. 49; no. 4; pp. 1148 - 1156
• Main Authors: Koike, Tatsuki, Constantinescu, Cristian C., Ikeda, Shuhei, Nishi, Toshiya, Sunahara, Eiji, Miyamoto, Maki, Cole, Patricia, Barret, Olivier, Alagille, David, Papin, Caroline, Morley, Thomas, Fowles, Krista, Seibyl, John, Tamagnan, Gilles, Kuroita, Takanobu
• Format: Journal Article
• Language: English
• Published: Berlin/Heidelberg Springer Berlin Heidelberg 01.03.2022; Springer Nature B.V
• Subjects: Animals; Autoradiography; Brain; Brain - diagnostic imaging; Brain - metabolism; Cardiology; Cerebellum; Cholesterol; Cholesterol 24-Hydroxylase - metabolism; Enzymes; Epilepsy; Fluorine isotopes; Homeostasis; Humans; Hydroxylase; Imaging; In vitro methods and tests; In vivo methods and tests; Macaca mulatta - metabolism; Medicine; Medicine & Public Health; Mice; Neostriatum; Neuroimaging; Nuclear Medicine; Occupancy; Oncology; Original; Original Article; Orthopedics; Piperidines; Positron emission; Positron emission tomography; Positron-Emission Tomography - methods; Pyridines; Radiology; Seizures; Tomography; CH24H; Soticlestat; [; Cholesterol 24-hydroxylase; F; PET; 18F

Purpose Cholesterol 24-hydroxylase (CH24H) is a brain-specific enzyme that plays a major role in brain cholesterol homeostasis by converting cholesterol into 24 S -hydroxycholesterol. The selective CH24H inhibitor soticlestat (TAK-935) is being pursued as a drug for treatment of seizures in developm...