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

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 α1A1B α1A1D α1B1D
(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.