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J Nucl Med. 2008; 49 (Supplement 1):288P
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Radiopharmaceutical Chemistry: New Chemistry-Neurosciences

New Chemistry-Neurosciences Posters

Synthesis and evaluation of 18F-MDL 100907 derivatives for the 5-HT2A receptor

Matthias Herth1, Markus Piel1, Fabian Debus2, Mikael Palner3 and Frank Roesch1

1 Institute of Nuclear Chemistry; 2 Psychiatry, University of Mainz, Mainz, Rheinland-Pfalz, Germany; 3 Center for Integrated Molecular Brain Imaging, Rigshospitalet, Copenhagen, Rheinland-Pfalz, Germany

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Objectives: The objective of this study was to develop 18F-analogs of MDL 10007 combining the advantages of the greater selectivity of MDL 100907 over Altanserin and the better isotopic properties of 18F compared to the existing [11C]MDL 100907.

Methods: Several MDL 100907 derivatives were synthesized and tested due to their affinities towards the 5-HT2A receptor. Most promising ligands were chosen to have replaced a methoxy- by a fluoroethoxy group and checked for their affinities towards the 5-HT2A receptor. Fluoroethyl derivatives of MDL 100907 (fig. 1) were synthesized via a fluoroalkylation in a yield of about 40%. [18F]fluoroalkylation of three compounds (MA15, MA15(R), MA48) were already synthesized. Finally, autoradiographic and PET studies were carried out.

Results: Reference compounds showed desired affinities of 0.7 to 9.0 nM towards the 5-HT2A receptor. As expected, the enantioselective compound MA15(R) ((R)-MHMZ; ((R)-2-fluoroethoxy-3-methoxyphenyl)-1-[2-(4-fluoro-phenyl)ethyl-4-piperidine-methanol) showed the highest affinity of 0.7 nM. Optimization of the radiochemical reaction conditions gave yields of about 80 – 90 % for he fluoroalkylation. The final formulation took no longer than 100 minutes and provided the labeled compounds with a purity > 96%. Autoradiographic and PET images showed excellent visualization results of the 5-HT2A receptor in the rat brain.

Conclusions: The new 18F-labeled compounds could be obtained as an injectable solution in radiochemical yields about 40% within a synthesis time of about 100 minutes in a purity of > 96%. In conclusion, our results justify further experiments to verify the potential of this new 5-HT2A imaging ligands.





This Article
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Right arrow Articles by Roesch, F.