Table 2.
No. | R | OX1 Ke (nM)a | OX2 Ke (nM)a or % inhibition at 10 μM |
---|---|---|---|
17a | n-Propyl | >10000 | b |
17b | 2,2,2-Trifluoroethyl | >10000 | b |
17c | iso-Propyl | >10000 | b |
17d | Benzyl | >10000 | b |
17e | 1000 ± 190c | b | |
17f | >10000 | b | |
18a | Methylsulfonyl | >10000 | 1330 ± 260 |
18b | Benzenesulfonyl | >10000 | b |
19 | Propionoyl | >10000 | 1290 ± 130 |
Ke values are the mean ± SEM of three independent experiments performed in duplicate. Results where Ke > 10 μM are N=2.
Less than 50% inhibition at 10 μM.
Pre-incubation of antagonist and test compound was 1 hr.