Non-peptidic 18F-labeled PET radiotracers for oxytocin receptor imaging
Oxytocin is a neurohypophysial peptide hormone, synthesized in the hypothalamus and stored in the posterior pituitary gland for release into the bloodstream. Beside its peripheral hormonal actions, it regulates as neurotransmitter a diverse range of CNS functions, including emotional, parental and sexual behaviors. Its receptor (OTR) is expressed in peripheral organs as well as in specific brain areas related to cognitive function and psychiatric diseases such as schizophrenia and depression. Moreover, it was shown that the oxytocinergic system is involved in cell proliferation in human neuro- and glioblastomas. So far, investigation of the distribution of OTR in living brain is hampered by the lack of suitable radiotracers. Thus, the development of a brain-penetrant PET ligand with high affinity and selectivity to the OTR would promote the development of non-invasive and quantitative imaging of OTR expression in healthy and diseased brain.
Ligand design based on an in house developed CoMFA model
18F-labeling of the new OTR PET tracer [18F]ABX163 in a two-step procedure
ABX Advanced Biochemical Compounds GmbH, Radeberg, Germany
B. Wenzel, J. Mollitor, W. Deuther-Conrad, S. Dukic-Stefanovic, M. Kranz, C. Vraka, R. Teodoro, R. Günther, C. K. Donat, F.-A. Ludwig, S. Fischer, R. Smits, W. Wadsak, M. Mitterhauser, J. Steinbach, A. Hoepping, P. Brust:
„Development of a novel nonpeptidic 18F-labeled radiotracer for in vivo imaging of oxytocin receptors with positron emission tomography“
J. Med. Chem. (2016), 59, 1800-1817.