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Automated Radiochemical Synthesis of [18F]3F4AP: A Novel PET Tracer for Imaging Demyelinating Diseases
Published on: May 29, 2017
Potential CRF1R PET imaging agents:
Dmitry Zuev1, Ronald J Mattson, Hong Huang
1Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA. dmitry.zuev@bms.com
Abstract:
A series of N-fluoroalkyl-8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethyl-N-alkylpyrazolo[1,5-a][1,3,5]triazin-4-amines were prepared and evaluated as potential CRF(1)R PET imaging agents. Optimization of their CRF(1)R binding potencies and octanol-phosphate buffer phase distribution coefficients resulted in discovery of analog 7e (IC(50)=6.5 nM, logD=3.5).
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