Page - (000321) - in Biomedical Chemistry: Current Trends and Developments

reported in Tables 3.3.7 and 3.3.8. Table 3.3.6: Binding affinity (Ki values) and metabolic stability (Clint and t1/2) of the rigidified and C-terminal-modified H-Phe-Phe-NH2 analogs a The stereochemistry of each diastereomer pair was estimated from the pharmacophore model. b IC50 value. Analog 40 was tested at a 2:1 ratio with analog 41. It was tested once, at six different concentrations, in triplicate. c The metabolic stability data are expressed as mean ± SD. d Clint = in vitro intrinsic clearance. e t1/2 = in vitro half-life. Table 3.3.7: Active uptake and permeability data for the methylated H-Phe-Phe-NH2 analogs.