Table 2. Antagonist potencies and selectivities of nuciferine (3a) and roemerine (3b) enantiomers for α1 receptor subtypes calculated from pIC50 curves.
pKb
a
|
K
b (nM) |
Subtype selectivity
b
|
|||||||
Compound | α1A | α1B | α1D | α1A | α1B | α1B | α1A/α1B | α1A/α1D | α1B/α1D |
(R)-Nuciferine | 7.42 ± 0.07 | 7.22 ± 0.01 | 6.78 ± 0.01 | 37.8 | 60.6 | 165 | 2 | 4 | 3 |
(S)-Nuciferine | 7.17 ± 0.08 | 6.50 ± 0.01 | 6.94 ± 0.01 | 67.1 | 316 | 116 | 5 | 2 | 0.4 |
(R)-Roemerine | 6.47 ± 0.08 | 6.57 ± 0.05 | 7.34 ± 0.15 | 338 | 266 | 46.0 | 0.8 | 0.1 | 0.2 |
(S)-Roemerine | 7.07 ± 0.01 | 6.81 ± 0.03 | 7.04 ± 0.07 | 86.0 | 154 | 92.2 | 2 | 1 | 0.6 |
Prazosin c | 9.69 ± 0.07 | 11.41 ± 0.09 | 10.60 ± 0.02 | 0.20 | 0.004 | 0.025 | 0.02 | 0.1 | 6 |
aValues are expressed as mean ± SEM from at least 2 separate experiments.
bSelectivities for receptor X/receptor Y were calculated as the ratio of Kb receptor Y/Kb receptor X.
cPositive control.