Table 1.
Affinity of MPC-6827 to Brain Targetsa
| targets | affinity (nM) | targets | affinity (nM) |
|---|---|---|---|
| MT | 1.531,32 | 5-HT1A-1E | >10000 |
| 5-HT2A-2C | >10000 | 5-HT3-7 | >10000 |
| 5-HT2A-2C | >10000 | A | >10000 |
| 5-HT3–7 | >10000 | α1A-1C | >10000 |
| α2A-2C | >10000 | β1–3 | >10000 |
| AMPA | >10000 | BZP | >10000 |
| Ca+ channel | >10000 | CB1, CB2 | >10000 |
| D1-D5 | >10000 | DAT | >10000 |
| DOR | >10000 | H1 | >10000 |
| H2 | 155 | H3, H4 | >10000 |
| HERG | >10000 | GABA | >10000 |
| EP | >10000 | I | >10000 |
| KOP | >10000 | KA | >10000 |
| M | >10000 | mGluR | >10000 |
| MDR1 | >10000 | MOR | 6479 |
| NET | >10000 | NK | >10000 |
| NMΔA | >10000 | NOP | >10000 |
| NT | >10000 | oxytocin | >10000 |
| PBR | >10000 | PKC | >10000 |
| SERT | >10000 | σ1 | 426 |
| σ2 | >10000 | Na + channel | >10000 |
| smoothened | >10000 | VMAT 1,2 | >10000 |
a
MT, microtubule; 5-HT, 5-hydroxytryptamin; A, adenosine; α, alpha; β,: beta; BZP, benzodiazepine; AMPA, R-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid; CB, cannabinoid; D, dopamine; DAT, dopamine transporters; DOR, δ opioid receptors; EP, prostanoid receptors: GABA, γ-amino butyric acid; H, histamine; hERG, human ether-a-go-go; KA, kainate; KOR, κ opioid receptors; M, muscarinic; MDR, multidrug resistance; MOR, μ opioid receptor; mGluR, metabotropic glutamate receptors; NMDA, N-methyl-D-aspartic acid; NK, neurokinin; NET, norepinephrine transporter; NT, neurotrophin; PKC, protein kinase C; SERT, serotonin transporter; V, vasopressin; VMAT, vesicular monoamine transporter.