Potential CRF1R PET imaging agents: N-fluoroalkyl-8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethyl-N-alkylpyrazolo[1,5-a][1,3,5]triazin-4-amines.

Dmitry Zuev, Ronald J. Mattson,Hong Huang,Gail K. Mattson,Larisa Zueva,Julia M. Nielsen,Edward S. Kozlowski,Xiaohua Stella Huang,Dedong Wu,Qi Gao,Nicholas J. Lodge,Joanne J. Bronson,John E. Macor

Bioorganic & Medicinal Chemistry Letters（2011）

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摘要

A series of N-(3-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 CRF1R PET imaging agents. Optimization of their CRF1R binding potencies and octanol-phosphate buffer phase distribution coefficients resulted in discovery of analog 7e (IC50=6.5nM, logD=3.5).

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关键词

Corticotropin-releasing factor,Imaging agents,Positron emission tomography,Anxiety,Depression

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