Table 1.
Selectivity of SAN4825 and SAN2589 against a panel of 33 proteins
| Assay | SAN2589 | SAN4825 |
|---|---|---|
| A1 (h) (antagonist radioligand) | 83 ± 3 | 72 ± 1 |
| A2A (h) (agonist radioligand) | 61 ± 6 | 19 ± 1 |
| Alpha 1A (antagonist radioligand) | 98 ± 7 | 94 ± 6 |
| Alpha 2A (h) (antagonist radioligand) | 92 ± 12 | 108 ± 5 |
| Beta 1 (h) (agonist radioligand) | 95 ± 1 | 93 ± 5 |
| Beta 2 (h) (agonist radioligand) | 104 ± 8 | 95 ± 12 |
| CB1 (h) (agonist radioligand) | 89 ± 24 | 89 ± 6 |
| CB2 (h) (agonist radioligand) | 101 ± 4 | 93 ± 1 |
| D1 (h) (antagonist radioligand) | 120 ± 1 | 116 ± 4 |
| D2S (h) (antagonist radioligand) | 107 ± 15 | 89 ± 4 |
| Glycine (strychnine-sensitive) (antagonist radioligand) | 109 ± 13 | 80 ± 6 |
| H1 (h) (antagonist radioligand) | 105 ± 10 | 98 ± 5 |
| H2 (h) (antagonist radioligand) | 119 ± 19 | 90 ± 4 |
| M1 (h) (antagonist radioligand) | 102 ± 3 | 88 ± 3 |
| M2 (h) (antagonist radioligand) | 114 ± 2 | 86 ± 8 |
| M3 (h) (antagonist radioligand) | 97 ± 0.4 | 81 ± 2 |
| N neuronal alpha 4beta 2 (h) (agonist radioligand) | 114 ± 10 | 93 ± 6 |
| N muscle-type (h) (antagonist radioligand) | 99 ± 6 | 96 ± 8 |
| Mu (MOP) (h) (agonist radioligand) | 104 ± 6 | 96 ± 16 |
| PCP (antagonist radioligand) | 103 ± 1 | 117 ± 8 |
| 5-HT1A (h) (agonist radioligand) | 97 ± 8 | 107 ± 10 |
| 5-HT2A (h) (antagonist radioligand) | 123 ± 14 | 98 ± 5 |
| 5-HT2B (h) (antagonist radioligand) | 103 ± 5 | 100 ±9 |
| Ca2+ channel (L, dihydropyridine site) (antagonist radioligand) | 118 ± 29 | 109 ± 0.2 |
| KV channel (antagonist radioligand) | 131 ± 6 | 93 ± 9 |
| SKCa channel (antagonist radioligand) | 88 ± 3 | 96 ± 0.4 |
| Cl− channel (GABA-gated) (antagonist radioligand) | 97 ± 1 | 89 ± 0 |
| Norepinephrine transporter (h) (antagonist radioligand) | 95 ± 1 | 102 ± 0.3 |
| dopamine transporter (h) (antagonist radioligand) | 103 ± 29 | 94 ± 5 |
| PDE3A (h) | 96 ± 2 | 90 ± 1 |
| Acetylcholinesterase (h) | 107 ± 2 | 89 ± 5 |
| MAO-A (h) | 98 ± 11 | 98 ± 3 |
| ATPase (Na+/K+) | 99 ± 1 | 103 ± 2 |
Compounds were tested in duplicates at 10 μM. Results shown are expressed as percent activity of control ± standard deviation