Table 1. Antagonist potencies and selectivities of nuciferine (3a) and roemerine (3b) enantiomers for 5-HT2 receptor subtypes calculated from pIC50 curves.
pKb
a
|
K
b (nM) |
Subtype selectivity
b
|
|||||||
Compound | 5-HT2A | 5-HT2B | 5-HT2C | 5-HT2A | 5-HT2B | 5-HT2C | 5-HT2A/5-HT2B | 5-HT2A/5-HT2C | 5-HT2C/5-HT2B |
(R)-Nuciferine | 7.18 ± 0.03 | 7.51 ± 0.21 | 7.44 ± 0.01 | 65.3 | 31.0 | 36.4 | 0.5 | 0.6 | 1 |
(S)-Nuciferine | 7.07 ± 0.17 | 7.38 ± 0.01 | 7.51 ± 0.22 | 84.3 | 41.7 | 41.7 | 0.5 | 0.4 | 1 |
(R)-Roemerine | 7.97 ± 0.18 | 7.08 ± 0.43 | 7.82 ± 0.08 | 10.8 | 84.0 | 15.1 | 8 | 1 | 6 |
(S)-Roemerine | 7.37 ± 0.10 | 7.03 ± 0.33 | 7.12 ± 0.13 | 42.9 | 92.7 | 76.9 | 2 | 2 | 1 |
Ketanserin c | 8.69 ± 0.03 | 5.70 ± 0.04 | 6.95 ± 0.08 | 2.0 | 1980 | 112 | 1000 | 60 | 20 |
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.