TABLE 1

Analytic and Affinity Data of GRPr Antagonists

Mass ([M+2H]+)
CompoundCalculatedMeasuredIC50 (nmol/L)
Ga-DOTA-AR906.4906.50.48 ± 0.18 (5)
Ga-HZ219971.0970.90.69 ± 0.18 (4)
Ga-HZ2201430.51430.421.4 ± 7.4 (6)
DOTA-RM2853.4853.77.7 ± 3.3
  • Values (mean ± SD) from binding studies were determined in PC-3 cells. Number of independent experiments is given in parentheses (triplicate measurements were performed in each experiment). Data for DOTA-RM2 are from Mansi et al. (15).