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11C-GSK189254 : a selective radioligand for in vivo central nervous system imaging of histamine H3 receptors by PET

The paper describes the in vivo characterisation of the first selective PET biomarker to imaging H3 receptors, labelled with the short-lived (20.4 min) positron emitting isotope carbon-11 and demonstrates that the compound warrants translation into humans. The H3 receptor is a drug target of considerable interest in the pathophysiology of Alzheimer’s disease and schizophrenia. The novel PET ligand has since been successfully translated to human imaging studies and is in use by several pharma companies in optimising drug dose-receptor occupancy relationships of new therapeutics for CNS disorders (see for example GSK: http://ichgcp.net/clinical-trials-registry/research/index/NCT00474513 and Johnson & Johnson, Psychopharmacology, 2012).