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

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, log  D  = 3.5).