Table 2.
Pharmacological profile of sites labeled by [125I]-E-IA-BF-PIPZE is consistent with selective radioligand binding to σ1 receptors in membranes from whole mouse braina,b
| Compound | IC50 (nM) | Ki (nM) | Hill (nH) |
|---|---|---|---|
| Haloperidol | 1.2 ± 0.2 | 0.9 ± 0.2 | 0.9 ± 0.1 |
| E-IA-BF-PIPZE | 1.7 ± 0.2 | 1.1 ± 0.1 | 1.0 ± 0.1 |
| (+)-Pentazocine | 13.7 ± 1.4 | 8.1 ± 0.8 | 0.9 ± 0.1 |
| BD1063 | 13.6 ± 0.7 | 9.6 ± 0.5 | 1.3 ± 0.1 |
| (+)-SKF10,047 | 43.2 ± 3.5 | 28.8 ± 2.4 | 1.1 ± 0.1 |
| DTG | 209 ± 14 | 114 ± 7 | 1.0 ± 0.1 |
| (−)-SKF10,047 | 7091 ± 519 | 5005 ± 366 | 1.3 ± 0.3 |
| Br-Mach | 9851 ± 807 | 6390 ± 524 | 1.1 ± 0.2 |
a
Values are means ± SEM (n = 3 – 6).
b
0.1 nM [125I]-E-IA-BF-PIPZE; 37 °C, 180 min; 50 mM TRIS, pH 8, 0.01% bovine serum albumin; 1.0 μM haloperidol defined non-specific binding.