Table 2.
Selective ligands for the dopamine D4 receptor
Ligand | Affinity for D4 (nM) | Specific purposes, uses, applications |
---|---|---|
L-745,870 | 0.43–0.51 | In vivo administration in rodents for functional, behavioural and drug-dependence studies [177–179]; development of PET radioligands [180]; in D4 receptor-overexpressing cell systems [52, 181]; tests for antipsychotic activity [120, 182] |
L-741,742 | 3.5 | In vivo administration to mice for anxiety testing [183] |
ABT 724 | ~45–65 | In vivo administration to rats to test potential treatment of erectile dysfunction [184, 185] |
WAY 100635 | 16.4 | D4 receptor agonist and 5HT1A antagonist; produces discriminative stimulus effects in rats [186, 187] |
PD 168077 | 8.7 | Selective D4 agonist, proerectile effect in rats [188]; tested in mice for memory consolidation studies [189] |
PNU 96415E | 3 | Tested for antipsychotic potential [190] |
Ro 10-5824 | 5.2 | Selective D4 agonist, increases novel exploration in mice [191] |
NGD 94-1 | 3 | In vivo administration to monkey for cognitive and memory tests [192]; in vitro autoradiography studies [193, 194] |
NRA 0160 | 0.5 | Tested for antipsychotic activity in animal models [195, 196] |
CI 1030 | 4.3 | Tested for antipsychotic activity in animal models [195, 196] |
A-412997 | 7.9 | D4 receptor agonist; improves cognitive performance and stimulates motor activity in rats [197] |