Table 3.
Off-Target Profiling of Three Alkaloids at ~50 CNS Human Receptors through PDSP
| (a) mitraciliatine PDSP screening | |
|---|---|
| target | affinity (Ki (pEC50 ± SEM) nMa |
| hNET | 6604 (5.2 ± 0.1) |
| hMOR | 304 (6.52 ± 0.06) |
| hKOR | 73 (7.14 ± 0.07) |
| hα2A | 2153 (5.67 ± 0.09) |
| (b) Isopaynantheine PDSP Screening | |
| hSERT | 5111 (5.3 ± 0.2) |
| hDAT | 5066 (5.3 ± 0.2) |
| hMOR | 122 (6.91 ± 0.07) |
| hKOR | 27 (7.57 ± 0.07) |
| hH1 | 206 (6.7 ± 0.1) |
| hα2A | 2152 (5.7 ± 0.1) |
| (c) Corynantheidine PDSP Screening | |
| h5HT1A | 1156 (5.96 ± 0.06) |
| hSERT | 2615 (5.6 ± 0.2) |
| hDAT | 3915 (5.4 ± 0.2) |
| hMOR | 339 (6.47 ± 0.07) |
| hKOR | 2109 (5.68 ± 0.07) |
| hH2 | 5126 (5.29 ± 0.07) |
| hα1A | 397 (6.4 ± 0.06) |
| hα1B | 3304 (5.48 ± 0.06) |
| hα2A | 74 (7.1 ± 0.1) |
| hα2B | 1539 (5.81 ± 0.08) |
| hα2C | 269 (6.57 ± 0.09) |
| hSigma 2 | 1073 (6 ± 0.1) |
| hNMDA | 83 (7.08 ± 0.09) |
a
National Institute of Mental Health Psychoactive Drug Screening Program (NIMH-PDSP) conducted the binding affinities reported in Table 3. The methods and radioligands details used for the binding assays are available on the NIMH PDSP website and Besnard et al., 2012, 492(7428), 215–20.