Table 1. Comparison of the Probes’ Affinity to α1-ARs.
Kia(nM) |
IC50 (nM) |
|||||
---|---|---|---|---|---|---|
compd | α1A | α1B | α1D | α1A | α1B | α1D |
phentolamine | 0.6 | 4.8 | 7.6 | 1.1 | 10.8 | 12.5 |
1a | 2.1 | NAc | NAc | 3.9 | <5b | <5b |
1b | 1.3 | NAc | NAc | 2.5 | <5b | <5b |
1c | 0.3 | 0.1 | 0.4 | 0.6 | 1.2 | 2.2 |
1d | 4.7 | 7.3 | 20.7 | 8.8 | 16.3 | 34.0 |
1e | 29.9 | 29.9 | 27.5 | 52.4 | 52.4 | 45.2 |
Ki was calculated from IC50 using the Cheng–Prusoff equation.
Data was estimated from the unclassical binding-competitive curve.
Not available.