{"doi":"10.3389/fmolb.2020.586327","title":"Synthesis and Characterization of Carbon-11 Labeled Iloperidone for Imaging of α1-Adrenoceptor in Brain","abstract":"α1-Adrenoceptor is implicated in numerous neuronal diseases. The development of new modulators targeting this receptor as well as the investigation of the role of α1-adrenoceptor in healthy and disease conditions, however, is hindered by the lack of specific positron emission tomography (PET) radiotracers. Iloperidone shows a high binding affinity to α1-adrenoceptor and moderate selectivity over other brain receptors. We report herein the synthesis and characterization of carbon-11 labeled iloperidone for imaging of α1-adrenoceptor in brain. The radiolabeling of [11C]iloperidone was carried out conveniently in one step by treating precursor with [11C]CH3I in DMF in the presence of K2CO3. Then, [11C]iloperidone was purified by semi-preparative HPLC, and characterized in C57BL/6 mice using PET/CT scanning. The desired product [11C]iloperidone was obtained in an average decay corrected radiochemical of 12% (n = 3) and over 99% radiochemical purity. The average molar radioactivity was 357 GBq/μmol with total synthetic time of 35-40 min. PET/CT scanning in C57BL/6 mice showed favorable pharmacokinetic properties and high brain exposure of [11C]iloperidone. Blocking experiments by pretreatment with the unlabeled iloperidone showed the significant blocking effects with about 25% reduction in brain uptake. These results suggested that [11C]iloperidone can serve as a lead compound for the further development of specific radiotracers for PET imaging α1-adrenoceptor in brain clinically.","journal":"Frontiers in Molecular Biosciences","year":2020,"id":85446,"datarank":0.29467882142690344,"base_score":1.9459101490553132,"endowment":1.9459101490553132,"self_citation_contribution":0.29188652235829704,"citation_network_contribution":0.0027922990686064146,"self_endowment_contribution":0.29188652235829704,"citer_contribution":0.0027922990686064146,"corpus_percentile":null,"corpus_rank":null,"citation_count":6,"citer_count":1,"citers_with_citation_signal":1,"citers_with_endowment":1,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9527,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2020-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":437274,"name":"Yanli Wang","orcid":"0000-0002-7576-3235","position":1,"is_corresponding":false},{"id":437275,"name":"Hao Wang","orcid":"0000-0001-7958-3090","position":2,"is_corresponding":false},{"id":329739,"name":"Changning Wang","orcid":"0000-0002-2076-4193","position":3,"is_corresponding":false},{"id":426549,"name":"Yulong Xu","orcid":"0000-0001-9024-7311","position":0,"is_corresponding":true}],"reference_count":19,"raw_metadata":{"citation_network_status":"fetched"},"created_at":"2026-07-18T21:58:16.217017Z","pmid":"33195432","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":[]}