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. 2011 Apr 15;21(8):2484-8.
doi: 10.1016/j.bmcl.2011.02.050. Epub 2011 Feb 17.

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  1 , 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
Affiliations

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 et al. Bioorg Med Chem Lett. .

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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