TABLE II.
Compound | IC50 (nM) | b Sigma1Ki (nM) | nH | IC50 (nM) | c Sigma2Ki (nM) | nH | Selectivity Ki Ratio σ2/σ1 |
---|---|---|---|---|---|---|---|
Ifenprodil | 35.03 ± 0.95 | 22.68 ± 0.61 | 1.08 ± 0.06 | 2.69 ± 0.36 | 2.43 ± 0.32 | 0.70 ± 0.07 | 0.1 |
(+)-Pentazocine | 7.88 ± 0.53 | 5.10 ± 0.34 | 1.09 ± 0.03 | 2280 ± 167 | 2060 ± 151 | 0.86 ± 0.04 | 404 |
DTG | 172.7 ± 19.88 | 111.8 ± 12.86 | 0.91 ± 0.14 | 43.3 ± 3.2 | 39.1 ± 2.8 | 0.88 ± 0.05 | 0.35 |
BD1063 | 9.68 ± 1.00 | 5.98 ± 0.62 | 1.17 ± 0.08 | 843 ± 104 | 762 ± 94 | 0.96 ± 0.13 | 127 |
(−)-Cocaine | 2074 ± 341 | 1347 ± 221 | 1.00 ± 0.11 | 53420 ± 4154 | 48170 ± 3748 | 1.03 ± 0.05 | 36 |
(−)-Cocained | 1359 ± 53 | 1075 ± 42 | 0.91 ± 0.11 | ||||
E-IA-DM-PE-PIPZE | 10.39 ± 1.39 | 6.73 ± 0.90 | 0.98 ± 0.07 | 1604 ± 243 | 1447 ± 220 | 0.98 ± 0.08 | 215 |
Dextromethorphan | 97.5 ± 6.9 | 63.1 ± 4.5 | 0.88 ± 0.07 | 29970 ± 2823 | 26810 ± 2525 | 1.02 ± 0.07 | 425 |
Haloperidol | 2.12 ± 0.22 | 1.35 ± 0.12 | 0.94 ± 0.03 | 80.7 ± 12.9 | 72.8 ± 11.6 | 1.12 ± 0.06 | 54 |
(+)-NANM | 20.55 ± 1.14 | 13.30 ± 0.74 | 1.06 ± 0.11 | 8991 ± 850 | 8095 ± 765 | 0.98 ± 0.12 | 608 |
(−)-NANM | 3985 ± 600 | 2551 ± 383 | 1.09 ± 0.08 | 7465 ± 469 | 6720 ± 422 | 0.93 ± 0.08 | 2.6 |
Values are means ± SEM, n = 3 – 6.
3.0 nM [3H](+)pentazocine, 37 °C, 180 min, 1.0 μM haloperidol defined non-specific binding.
3.0 nM [3H]DTG/500 nM (+)pentazocine, 25 °C, 60 min, 10.0 μM haloperidol defined non-specific binding.
1.0 nM [125I]E-IA-DM-PE-PIPZE, 37 °C, 60 min, 1.0 μM haloperidol defined non-specific binding.