Table 3.
M. speciosa alkaloid concentration | δ-opioid | κ-opioid | μ-opioid |
---|---|---|---|
corynoxine (1) | |||
100 nM | −3.9 | 3.8 | 80.1 |
10 000 nM | 73.8 | 75.3 | 97.8 |
corynoxine B (2) | |||
100 nM | −4.4 | 4.5 | 45.4 |
10 000 nM | 65.5 | 51.8 | 94.4 |
isospeciofoline (3) | |||
100 nM | 0.0 | 0.1 | 13.1 |
10 000 nM | 27.1 | 37.3 | 83.3 |
mitragynine oxindole B (4) | |||
100 nM | 10.4 | 5.0 | 7.3 |
10 000 nM | 87.1 | 23.0 | 66.5 |
speciociliatine N(4)-oxide (10) | |||
100 nM | 5.1 | 6.6 | 10.5 |
10 000 nM | 53.5 | 80.9 | 84.6 |
For subtype δ, human recombinant Chem-1 (RBL) cells. [3H]DADLE at 0.5 nM was used as a ligand. Naltrexone (10 μM) was used as a nonspecific binder, with 60 min incubation. For subtype κ, human recombinant RBL cells. [3H]U69,593 at 0.5 nM was used as a ligand. Naloxone (10 μM) was used as a nonspecific binder, with 60 min incubation. For subtype μ, human recombinant HEK-293 cells. [3H]DAMGO at 0.5 nM was used as a ligand. Naloxone (10 μM) was used as a nonspecific binder, with 120 min incubation. All assays were performed at room temperature.
Bold font in body of the table represents >50% displacement.