849469-03-0Relevant articles and documents
Synthesis and in vitro/in vivo pharmacological evaluation of [ 11C]-ThioABP, a novel radiotracer for imaging mGluR5 with PET
Sephton, Selena Milicevic,Mu, Linjing,Müller, Adrienne,Wanger-Baumann, Cindy A.,Schibli, Roger,Kr?mer, Stefanie D.,Ametamey, Simon M.
, p. 520 - 526 (2013/04/24)
We have designed a novel positron emission tomography (PET) radiotracer, [11C]-ThioABP, a thiazole based derivative for imaging the metabotropic glutamate receptor subtype 5 (mGluR5), and prepared the hydroxy oxime precursor 4 in a 15% overall yield. [11C]-ThioABP was radiosynthesized in the Veenstra module and obtained in a decay corrected radiochemical yield of 40% and specific activity of 80-250 GBq μmol -1 at the end of synthesis. ThioABP exhibited excellent binding affinity (Ki) in vitro of 1.9 ± 0.9 nM and [ 11C]-ThioABP showed an optimal log D7.4 of 2.4. The autoradiographic studies on rat brain slices revealed specific binding to mGluR5. In vivo evaluation of [11C]-ThioABP including a displacement study with MMPEP in a dynamic PET scan showed a specificity of [ 11C]-ThioABP for mGluR5. Radio-TLC metabolite studies showed a good metabolic stability of [11C]-ThioABP in vivo. The comparison of biological properties of [11C]-ThioABP and [11C]-ABP688 revealed similarity between these two compounds.
PYRIDYLACETYLENES FOR USE AS RADIOTRACERS AND IMAGING AGENTS
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Page/Page column 4-5, (2008/06/13)
The present invention relates to novel pyridylacetylene derivatives of formula I, their Preparation, their use as radiotracers/markers and compositions containing them.