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. 2018 Feb 26;9(3):576–582. doi: 10.1039/c7md00629b

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.