Table 3. Antagonist potencies and selectivities of nuciferine (3a) and roemerine (3b) enantiomers for 5-HT2A and α1A receptors determined from Schild analysis.
pKb
a
|
5-HT2A/α1A selectivity b | ||
Compound | 5-HT2A | α1A | |
(R)-Nuciferine | 7.26 ± 0.12 | 7.31 ± 0.11 | 1 |
(S)-Nuciferine | 6.85 ± 0.14 | 6.91 ± 0.07 | 1 |
(R)-Roemerine | 7.88 ± 0.13 | 6.38 ± 0.11 | 32 |
(S)-Roemerine | 7.06 ± 0.11 | 6.62 ± 0.11 | 3 |
aValues are expressed as mean ± SD.
bSelectivities for receptor X/receptor Y were calculated as the ratio of Kb receptor Y/Kb receptor X.