Compounds | Pituitary Mean Ki | Cortex Mean Ki | Pituitary/Cortex MeanKi Ratio | Significance (pValues) (n) |
---|---|---|---|---|
nM | ||||
SN003 | 7.9 ± 0.8 | 2.5 ± 0.4 | 3.4 ± 0.5 | **0.001 (6) |
DMP696 | 2.6 ± 0.5 | 1.0 ± 0.1 | 2.5 ± 0.6 | *0.017 (6) |
α-helical CRF | 8.1 ± 2.3 | 5.3 ± 1.9 | 3.3 ± 2.8 | 0.222 (9) |
hrCRF | 0.6 ± 0.1 | 0.7 ± 0.2 | 0.9 ± 0.3 | 0.388 (6) |
Parallel competition assays were conducted to generate IC50values of compounds inhibiting 50% of [125I]oCRF (200 pM) binding to rat pituitary and cortical membranes. Data shown are the mean Ki (± S.E.M.) from six to nine experiments performed in duplicate. The number of independent paired experiments performed is shown in parentheses. The statistical significance of Ki values of compounds between cortex and pituitary was assessed by a paired Student's t test, and two-tailed p values (∗, <0.05) were considered as significant.