1224432-91-0Relevant academic research and scientific papers
Fluorinated pyridylacetylene derivatives as tracers
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Page/Page column 8, (2014/01/08)
The invention relates to a novel compound of formula (I) wherein F is 19F or 18F, in free base or acid addition salt form. In its radioactive form with 18F, the compound is useuful as a marker for radioimaging of brain and
Development of [18F]-PSS223 as a PET tracer for imaging of metabotropic glutamate receptor subtype 5 (mGluR5)
Sephton, Selena Milicevic,Dennler, Patrick,Leutwiler, Dominique S.,Mu, Linjing,Schibli, Roger,Kraemer, Stefanie D.,Ametamey, Simon M.
scheme or table, p. 201 - 204 (2012/07/28)
Involvement of metabotropic glutamate receptor subtype 5 (mGluR5) in physiological and pathophysiological processes in the brain has been demonstrated, and hence mGluR5 has emerged as an important drug target. [ 11C]-ABP688 is clinically the mo
Structure-activity relationships of fluorinated (E)-3-((6-Methylpyridin-2- yl)ethynyl)cyclohex-2-enone- O -methyloxime (ABP688) derivatives and the discovery of a high affinity analogue as a potential candidate for imaging metabotropic glutamate recepors subtype 5 (mGluR5) with Positron Emission Tomography (PET)
Baumann, Cindy A.,Mu, Linjing,Johannsen, Sinja,Honer, Michael,Schubiger, Pius A.,Ametamey, Simon M.
supporting information; experimental part, p. 4009 - 4017 (2010/08/06)
The metabotropic glutamate receptor subtype 5 (mGluR5) is recognized to be involved in numerous brain disorders. In an effort to obtain a fluorine-18 labeled analogue of the mGluR5 PET tracer [11C]ABP688, 13 novel ligands based on the core structure of ABP688 were synthesized. Molecules in which the methyl group at the oxime functionality of ABP688 was replaced by fluorobenzonitriles, fluoropyridines, and fluorinated oxygen containing alkyl side chains were investigated. Substituents at the oxime functionality are well tolerated and resulted in five candidates with Ki values below 10 nM. The most promising candidate, (E)-3-(pyridin-2-ylethynyl)cyclohex-2-enone-O-2- (2-fluoroethoxy)ethyloxime (38, Ki = 3.8 nM), was radiolabeled with fluorine-18. Scatchard analysis of [18F]38 which modeled best for two sites pointed to high binding affinity (KD1 = 0.61 ± 0.19 nM and KD2 = 13.73 ± 4.69 nM) too. These data strongly suggest the further evaluation of [18F]38 as a candidate for imaging the mGluR5.
