{"doi":"10.62347/ivxm3055","title":"Radiosynthesis and evaluation of a carbon-11 labeled PET ligand for imaging of O-GlcNAcase","abstract":"O-GlcNAcase (OGA) is a key enzyme involved in regulating the dynamic cycling of O-GlcNAc modifications on intracellular proteins.OGA has emerged as a promising therapeutic target for neurodegenerative diseases, including Alzheimer's disease.In this report, we present the radiosynthesis and preclinical assessment of a novel carbon-11 labeled positron emission tomography (PET) radioligand [ 11 C]1 (codenamed OGA-2504) targeting OGA.The aminopyrimidine-based compound 1 and its corresponding desmethyl precursor were synthesized efficiently with good chemical yields.Radiosynthesis of [ 11 C]1 was accomplished via 11 C-methylation, yielding an 8% decaycorrected radiochemical yield with high purity (>98%) and high molar activity (92.5 GBq/mol).[ 11 C]1 exhibited moderate lipophilicity (LogD = 2.11) and excellent in vivo stability in serum.However, preliminary PET imaging revealed low brain uptake and slow clearance of [ 11 C]1 in mice, suggesting a need for further structural optimization to enhance brain penetration.","journal":"American Journal of Nuclear Medicine and Molecular Imaging","year":2025,"id":579602,"datarank":0.0,"base_score":0.0,"endowment":0.0,"self_citation_contribution":0.0,"citation_network_contribution":0.0,"self_endowment_contribution":0.0,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":0,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9596,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2025-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":1120882,"name":"Yinlong Li","orcid":"0000-0002-8864-1712","position":0,"is_corresponding":true}],"reference_count":0,"raw_metadata":null,"created_at":"2026-07-19T02:58:34.718602Z","pmid":"41280565","pmcid":null,"fwci":null,"citation_percentile":null,"influential_citations":0,"oa_status":null,"license":null,"views":0,"total_file_size_bytes":0,"version_count":0,"fair_f":null,"fair_a":null,"fair_i":null,"fair_r":null,"fair_zscore":null,"fair_rationale":null,"fair_model":null,"fair_agent_version":null,"fair_fulltext_source":null,"fair_has_llm":null,"fair_computed_at":null,"clinical_trials":[],"software_tools":[],"db_accessions":[],"linked_datasets":[],"topics":[]}