1304777-34-1Relevant articles and documents
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
Zuev, Dmitry,Mattson, Ronald J.,Huang, Hong,Mattson, Gail K.,Zueva, Larisa,Nielsen, Julia M.,Kozlowski, Edward S.,Huang, Xiaohua Stella,Wu, Dedong,Gao, Qi,Lodge, Nicholas J.,Bronson, Joanne J.,MacOr, John E.
, p. 2484 - 2488 (2011)
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 CRF1R PET imaging agents. Optimization of their CRF 1R binding potencies and octanol-phosphate buffer phase distribution coefficients resulted in discovery of analog 7e (IC50 = 6.5 nM, log D = 3.5).