Table 1.
Ki estimates for amisulpride at a large panel of cloned receptors
| Receptor | Ki | Radioligand | Incubation Buffer |
Incubation Time |
|---|---|---|---|---|
| 5-HT1A | > 10,000 nM | .5 nM [3H]8-OH-DPAT | SBB | 1.5 hours |
| 5-HT1B | 1744 ± 199 nM | .3 nM [3H]5-CT | SBB | 1.5 hours |
| 5-HT1D | 1341 ± 217 nM | .3 nM [3H]5-CT | SBB | 1.5 hours |
| 5-HT1E | > 10,000 nM | 3 nM [3H]5-HT | SBB | 1.5 hours |
| 5-HT2A | 8304 ± 1579 nM | .5 nM [3H]ketanserin | SBB | 1.5 hours |
| 5-HT2B | 13 ± 1.12 nM | 1.1 nM [3H]LSD | SBB | 1.5 hours |
| 5-HT2C | > 10,000 nM | .5 nM [3H]N-methyl-mesulergine | SBB | 1.5 hours |
| 5-HT3 | > 10,000 nM | .29 nM [3H]LY278584 | SBB | 1.5 hours |
| 5-HT5A | > 10,000 nM | 1 nM [3H]LSD | SBB | 1.5 hours |
| 5-HT6 | 4154 ± 599 nM | 1.05 nM [3H]LSD | SBB | 1.5 hours |
| 5-HT7 | 11.5 ± .71 nM | 1.05 nM [3H]LSD | SBB | 1.5 hours |
| 5-HT7a | 135.5 ± 15.8 nM | .35 nM [3H]5-CT | SBB | 1.5 hours |
| α1a | > 10,000 nM | .1 nM [125I]HEAT | A1BB | 1 hour |
| α1b | > 10,000 nM | .1 nM [125I]HEAT | A1BB | 1 hour |
| α1d | > 10,000 nM | .1 nM [125I]HEAT | A1BB | 1 hour |
| α2a | 1114 ± 124 nM | .1 nM [125I]clonidine | A2BB | 1 hour |
| α2c | 1540 ± 171 nM | .1 nM [125I]clonidine | A2BB | 1 hour |
| β1 | > 10,000 nM | .1 nM [125I]iodopindolol | BBB | 1 hour |
| β2 | > 10,000 nM | .1 nM [125I]iodopindolol | BBB | 1 hour |
| β3 | > 10,000 nM | .1 nM [125I]iodopindolol | BBB | 1 hour |
| Benzodiazapene | > 10,000 nM | .5 nM [3H]flunitrazepam | BZPBB | 1.5 hours |
| D1 | > 10,000 nM | .21 nM [3H]SCH23390 | DBB | 1.5 hours |
| D2 | 3 ± 1 nM | .19 nM [3H]N-methyl-spiperone | DBB | 1.5 hours |
| D3 | 3.5 ± .5 nM | .35 nM [3H]N-methyl-spiperone | DBB | 1.5 hours |
| D4 | 2369 ± 608 nM | .19 nM [3H]N-methyl-spiperone | DBB | 1.5 hours |
| D5 | > 10,000 nM | .21 nM [3H]SCH23390 | DBB | 1.5 hours |
| DOR | > 10,000 nM | .3 nM [3H]DADLE | SBB | 1.5 hours |
| KOR | > 10,000 nM | .3 nM [3H]U69593 | SBB | 1.5 hours |
| MOR | > 10,000 nM | .3 nM [3H]DAMGO | SBB | 1.5 hours |
| H1 | > 10,000 nM | .9 nM [3H]pyrilamine | HBB | 1.5 hours |
| H2 | > 10,000 nM | 3 nM [3H]tiotidine | HBB | 1.5 hours |
| H4 | > 10,000 nM | 5 nM [3H]histamine | HBB | 1.5 hours |
| M1 | > 10,000 nM | .5 nM [3H]QNB | MBB | 1.5 hours |
| M2 | > 10,000 nM | .5 nM [3H]QNB | MBB | 1.5 hours |
| M3 | > 10,000 nM | .5 nM [3H]QNB | MBB | 1.5 hours |
| M4 | > 10,000 nM | .5 nM [3H]QNB | MBB | 1.5 hours |
| M5 | > 10,000 nM | .5 nM [3H]QNB | MBB | 1.5 hours |
| DAT | > 10,000 nM | .5 nM [3H]WIN35428 | TBB | 1.5 hours |
| NET | > 10,000 nM | .5 nM [3H]nisoxetine | TBB | 1.5 hours |
| SERT | > 10,000 nM | .5 nM [3H]citalopram | TBB | 1.5 hours |
| EP3 | > 10,000 nM | .5 nM [3H]PGE2 | PBB | 1.5 hours |
| EP4 | > 10,000 nM | .5 nM [3H]PGE2 | PBB | 1.5 hours |
| σ1 | > 10,000 nM | 3 nM [3H]pentazocine | SigmaBB | 2.5 hours |
| σ2 | > 10,000 nM | 3 nM [3H]DTG | SigmaBB | 2.5 hours |
Standard Binding Buffer (SBB): 50 mM Tris HCl, 10 mM MgCl2, 0.1 mM EDTA, pH 7.4
Dopamine Binding Buffer (DBB): 50 mM HEPES, 50 mM NaCl, 5 mM MgCl2, 0.5 mM EDTA, pH 7.4
Histamine Binding Buffer (HBB): 50 mM Tris HCl, 0.5 mM EDTA, pH 7.4
Transporter Binding Buffer (TBB): 50 mM Tris HCl, 150 mM NaCl, 5 mM KCl, pH 7.4
Prostaglandin Binding Buffer (PBB): 25 mM Tris HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4
Alpha1 Binding Buffer (A1BB): 20 mM Tris HCl, 145 mM NaCl, pH 7.4
Alpha2 Binding Buffer (A2BB): 50 mM Tris HCl, 5 mM MgCl2, pH 7.7
Beta Binding Buffer (BBB): 50 mM Tris HCl, 3 mM MnCl2, pH 7.7
Muscarinic Binding Buffer (MBB): 50 mM Tris HCl, pH 7.7
Sigma Binding Buffer (SigmaBB): 50 mM Tris HCl, pH 8.0
Benzodiazapene Binding Buffer (BZPBB): 50 mM Tris HCl, 2.5 mM CaCl2, pH 7.4