title: Pharmacological prerequisites for PET ligands and practical issues in preclinical PET research.
abstract: The development of PET radiopharmaceuticals for the non-invasive imaging of cancerous lesions, brain receptors, transporters and enzymes started more than 25 years ago. But till today no established algorithms exist to predict the success of a PET radiopharmaceutical. PET radioligand development is a challenging endeavor and predicting the success of PET ligand can be an elusive undertaking. A large number of PET radiopharmaceuticals have been developed for imaging, but so far only a few have found application as imaging agents in vivo in humans. Typically, the potential compound selected for development usually has the desired in vitro characteristics but unknown in vivo properties. The purpose of this chapter is to highlight some of the pharmacological constraints and prerequisites. Interspecies difference in metabolism and mass effects are discussed with examples. Finally, some of the practical issues related to laboratory animal imaging using anesthetic agents are also presented.
authors.affiliation: Animal Imaging Center-PET, Center for Radiopharmaceutical Science of ETH, PSI and USZ, Zürich, Switzerland. simon.ametamey@pharma.ethz.ch
authors.forename: S M
authors.initials: SM
authors.lastname: Ametamey
authors.forename: M
authors.initials: M
authors.lastname: Honer
mesh_terms: D000758:Anesthesia; D000818:Animals; D004353:Drug Evaluation, Preclinical; D006801:Humans; D008024:Ligands; D049268:Positron-Emission Tomography / Q000379:methods*; D019275:Radiopharmaceuticals / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*
chemical_list: D008024:Ligands; D019275:Radiopharmaceuticals