Table 2. In vitro affinity findings lacking functional measurements.
| PDSP Hits Without Functional Assay | In vitro Affinity (nM) Radioligand used |
|---|---|
| 5-HT1D | 518 [3H]5-CT |
| α1A | 1386 [3H]Prazosin |
| α1B | 1995.3 [3H]Prazosin |
| α1D | 818 [3H]Prazosin |
| α2A | 1153.5 [3H]Rauwolscine |
| α2B | 686.8 [3H]Rauwolscine |
| α2C | 692.8 [3H]Rauwolscine |
| β1-AR | 7149 [3H]CGP12177 |
| β3-AR | 1103 [3H]CGP12177 |
| DOR | 10000 [3H]DADLE |
| H2 | 1662 [3H]Cimetidine |
| MOR | 9549.00 [3H]DAMGO |
| V1A | 10000 [3H]Vasopressin |
| 5-HT5A | 1113 [3H]LSD |
Receptor targets not predicted by SEA but identified by in vitro competition binding assays for which functional assays are not available. The following receptors assayed in the PDSP screen had no observed binding of nuciferine. Receptors are listed with their associated radioligand in (). Sets of receptors using the same radioligand are indicated in []: [5-HT1B, 5-HT1E]([3H]5-CT), 5-HT3 ([3H]GR65630), β2-AR ([3H]CGP12177), BZP Rat Brain Site ([3H]Flunitrazepam), D5([3H]SCH23390), DAT([3H]WIN35428), GabaA ([3H]Muscimol), H1 ([3H]Pyrilamine), H3 ([3H]α-methylhistamine), H4 ([3H]Histamine), KOR ([3H]U69593), NMDA PCP site ([3H]MK801), [M1, M2, M3, M4, M5]([3H]QNB or [3H]NMS), NET ([3H]Nisoxetine), Oxytocin([3H]Oxytocin), SERT ([3H]Citalopram), Sigma 1 ([3H]Pentazocine), Sigma 2 ([3H]DTG), [V1B, V2]([3H]Vasopressin).