Table 1. Functional and Radioligand Binding Data Obtained for NT, 1, 5a, 5b, and 6 at the NTS1 and NTS2 Receptors.
FLIPR assay |
bindinga | ||||||
---|---|---|---|---|---|---|---|
NTS1 |
NTS2 |
NTS2 | |||||
compd | EC50b | Emaxc | Ke | EC50 | Emaxd | IC50 | Ki |
NT | 0.04 ± 0.012 | 100 ± 3 | NAe | 18.5 ± 1.2 | 18.9 ± 3 | ||
1 | 0.01 ± 0.002 | 114 ± 7 | NA | 5.4 ± 0.6 | 33 ± 11 | ||
5a | 4.7 ± 0.8 | 120 ± 20 | 100 ± 3 | 62 ± 35 | |||
5b | 1.5 ± 0.6 | 20 ± 5 | 100 ± 5 | 6 ± 2 | |||
6 | NA | NA | 28 ± 4 | 16 ± 3 | 33 ± 5 |
[125I]NT,
EC50, Ke, IC50, and Ki values are nM ± SEM.
Emax value is % NT.
Emax value is % 5b.
Not active.