Publication: Evaluation of 5H-Thiazolo[3,2-α]pyrimidin-5-ones as Potential GluN2A PET Tracers
Evaluation of 5H-Thiazolo[3,2-α]pyrimidin-5-ones as Potential GluN2A PET Tracers
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He, Y., Whitehead, D. M., Briard, E., Numao, S., Mu, L., Schibli, R., Ametamey, S. M., & Auberson, Y. P. (2020). Evaluation of 5H-Thiazolo[3,2-α]pyrimidin-5-ones as Potential GluN2A PET Tracers. ChemMedChem, 15(24), 2448–2461. https://doi.org/10.1002/cmdc.202000340
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We describe here our efforts to develop a PET tracer for imaging GluN2A-containing NMDA receptors, based on a 5H-thiazolo[3,2-α]pyrimidin-5-one scaffold. The metabolic stability and overall properties could be optimized satisfactorily, although binding affinities remained a limiting factor for in vivo imaging. We nevertheless identified 7-(((2-fluoroethyl)(3-fluorophenyl)amino)-methyl)-3-(2-(hydroxymethyl)cyclopropyl)-2-methyl-5H-thiazolo-[3,2-α]pyrimidin-5-one ([18 F]7b) as a radioligand providing good-quality images in autoradiograp
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- He, Yingfang
- Whitehead, David M
- Briard, Emmanuelle
- Numao, Shin
- Mu, Linjing
- Schibli, Roger
- Ametamey, Simon M
- Auberson, Yves P
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He, Y., Whitehead, D. M., Briard, E., Numao, S., Mu, L., Schibli, R., Ametamey, S. M., & Auberson, Y. P. (2020). Evaluation of 5H-Thiazolo[3,2-α]pyrimidin-5-ones as Potential GluN2A PET Tracers. ChemMedChem, 15(24), 2448–2461. https://doi.org/10.1002/cmdc.202000340