New Isotope-Labelling Technique Published in JACS

Collaboration between researchers at iNANO and Aarhus University Hospital published in the Journal of the American Chemical Society.

Stig Friis, Thomas L. Andersen and Troels Skrydstrup

Researchers at the Interdisciplinary Nanoscience Center and the Department of Chemistry have devised a new isotope-labelling technique for pharmaceutically relevant molecules, which could assist in the development of new pharmaceuticals on the market.

The team consisting of PhD students Thomas L. Andersen and Stig Friis in the group of Professor Troels Skrydstrup has teamed up with Dr. Hélène Audrain from the Positron Emission Tomography (PET) Center at Aarhus University Hospital and have together developed efficient synthetic methodology for the carbon-11 labelling of three different structurally challenging pharmaceuticals.

This included a D2/D3 receptor antagonist, an antitumor agent for the treatment of ovarian cancer, and a neuropeptide Y Y2 receptor antagonist. The technique could assist drug development programs for understanding the fate of pharmaceuticals after administration to a patient (e.g. distribution, metabolic stability, target selectivity). Particularly challenging with this type of isotope-labelling is the short half life of carbon-11 being app. 20 minutes, requiring extremely rapid chemical reactions.

The methodology was also successfully implemented at the PET center, Uppsala University Hospital with PET chemists Dr. Gunnar Antoni and Dr. Patrik Nordeman. The work was published in the Journal of the American Chemical Society and was also highlighted by the journal.
(http://pubs.acs.org/doi/abs/10.1021/ja511441u)