Compound | [125I]DAIZAC1-a Rat BrainKi (± S.E.M.) (nH)1-d | [125I]DAIZAC1-bNCB-20 Cells Ki (± S.E.M.) (nH)1-d | [125I]IZAC1-c Rat Brain Ki | Reported ValueKi | Reference |
---|---|---|---|---|---|
nm | nm | ||||
Antagonists | |||||
DAIZAC | 0.14 ± 0.01 (0.95) | 0.14 ± 0.02 (1.05) | 0.13 | 0.15 | Mason et al., 1996 |
(S)-Zacopride | 0.22 ± 0.03 (0.98) | 0.16 ± 0.03 (1.01) | 0.24 | 0.22 | Wong et al., 1993 |
LY-278584 | 0.69 ± 0.03 (1.03) | 0.92 ± 0.12 (1.02) | 0.78 | 0.71 | Schmidt et al., 1990 |
(S)-Iodozacopride | 1.05 ± 0.09 (1.00) | 1.23 ± 0.05 (1.02) | 1.1 | 2.61-e | Ponchant et al., 1991 |
Bemesetron | 19.8 ± 5.4 (0.96) | 9.1 ± 1.9 (0.96) | 11 | 12 | Barnes et al., 1990 |
Mianserin | 56 ± 6 (0.95) | 120 ± 77 (0.96) | 130 | 81 | Barnes et al., 1990 |
Clozapine | 197 ± 10 (1.01) | 35 ± 15 (0.87) | 49 | Schmidt et al., 1990 | |
Metoclopramide | 201 ± 26 (0.97) | 124 ± 45 (0.96) | 282 | Wong et al., 1993 | |
Agonists | |||||
Quipazine | 0.83 ± 0.07 (1.72) | 2.1 ± 0.5 (0.96) | 1.8 | 1.4 | Wong et al., 1993 |
mCPBG | 3.2 ± 0.8 (1.30) | 29 ± 5 (1.27) | 3.0 | Laporte et al., 1992 | |
mCPP | 21 ± 3 (0.78) | 78 ± 8 (0.70) | 44 | Barnes et al., 1990 | |
PBG | 52 ± 5 (1.14) | 542 ± 76 (0.84) | 83 | Barnes et al., 1990 | |
2-Me-5-HT | 120 ± 2 (1.59) | 750 ± 216 (2.27) | 135 | Wong et al., 1993 | |
5-HT | 369 ± 78 (1.76) | 214 ± 13 (0.97) | 260 | Schmidt et al., 1990 |
Ki was calculated from IC50 values. Data represent the average of triplicate determinations from at least two experiments.
↵1-a Displacement of 0.1 nM [125I]DAIZAC binding in whole rat brain membranes.
↵1-b Displacement of 0.1 nM [125I]DAIZAC binding in NCB-20 cell membranes.
↵1-c Displacement of 0.4 nM (S)-[125I]iodozacopride ([125I]IZAC) binding in rat brain.
↵1-d nH is the pseudo-Hill slope of the displacement curve.
↵1-e Value for the racemic compound.