{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"omics_type":["Unknown"],"volume":["49(4)"],"submitter":["Koike T"],"pubmed_abstract":["<h4>Purpose</h4>Cholesterol 24-hydroxylase (CH24H) is a brain-specific enzyme that plays a major role in brain cholesterol homeostasis by converting cholesterol into 24S-hydroxycholesterol. The selective CH24H inhibitor soticlestat (TAK-935) is being pursued as a drug for treatment of seizures in developmental and epileptic encephalopathies. Herein, we describe the successful discovery and the preclinical validation of the novel radiolabeled CH24H ligand (3-[<sup>18</sup>F]fluoroazetidin-1-yl){1-[4-(4-fluorophenyl)pyrimidin-5-yl]piperidin-4-yl}methanone ([<sup>18</sup>F]T-008) and its tritiated analog, [<sup>3</sup>H]T-008.<h4>Methods</h4>In vitro autoradiography (ARG) studies in the CH24H wild-type (WT) and knockout (KO) mouse brain sections were conducted using [<sup>3</sup>H]T-008. PET "],"journal":["European journal of nuclear medicine and molecular imaging"],"pagination":["1148-1156"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC8921165"],"repository":["biostudies-literature"],"pubmed_title":["Preclinical characterization of [<sup>18</sup>F]T-008, a novel PET imaging radioligand for cholesterol 24-hydroxylase."],"pmcid":["PMC8921165"],"pubmed_authors":["Koike T","Kuroita T","Ikeda S","Miyamoto M","Seibyl J","Fowles K","Constantinescu CC","Papin C","Nishi T","Barret O","Cole P","Alagille D","Sunahara E","Morley T","Tamagnan G"],"additional_accession":[]},"is_claimable":false,"name":"Preclinical characterization of [<sup>18</sup>F]T-008, a novel PET imaging radioligand for cholesterol 24-hydroxylase.","description":"<h4>Purpose</h4>Cholesterol 24-hydroxylase (CH24H) is a brain-specific enzyme that plays a major role in brain cholesterol homeostasis by converting cholesterol into 24S-hydroxycholesterol. The selective CH24H inhibitor soticlestat (TAK-935) is being pursued as a drug for treatment of seizures in developmental and epileptic encephalopathies. Herein, we describe the successful discovery and the preclinical validation of the novel radiolabeled CH24H ligand (3-[<sup>18</sup>F]fluoroazetidin-1-yl){1-[4-(4-fluorophenyl)pyrimidin-5-yl]piperidin-4-yl}methanone ([<sup>18</sup>F]T-008) and its tritiated analog, [<sup>3</sup>H]T-008.<h4>Methods</h4>In vitro autoradiography (ARG) studies in the CH24H wild-type (WT) and knockout (KO) mouse brain sections were conducted using [<sup>3</sup>H]T-008. PET ","dates":{"release":"2022-01-01T00:00:00Z","publication":"2022 Mar","modification":"2025-04-04T07:44:38.358Z","creation":"2025-04-04T07:44:38.358Z"},"accession":"S-EPMC8921165","cross_references":{"pubmed":["34651220"],"doi":["10.1007/s00259-021-05565-z"]}}