Table 3.
Agonist efficacy parameters
| pKi (Na+, GTP) | EC50 (Na+) | Ki/EC50 | pKi (NMDG, GTP) | EC50 (NMDG) | Ki/EC50 (NMDG) | |
|---|---|---|---|---|---|---|
| AJ-76 | 6.50 | 7.02 | 3.3 | 5.20 | 6.67 | 29.5 |
| Aplindore | 9.03 | 9.57 | 3.5 | 8.40 | 9.47 | 11.7 |
| Aripiprazole | 8.96 | — | — | 8.56 | 8.90 | 2.2 |
| Dopamine | 5.28 | 6.56 | 19.1 | 5.38 | 7.10 | 53.7 |
| (−)-3-PPP | 6.23 | 6.81 | 3.8 | 5.63 | 6.64 | 10.2 |
| UH-232 | 7.14 | — | — | 6.03 | 7.34 | 20.4 |
Abbreviations: AJ-76, (1S,2R)-cis-5-methoxy-1-methyl-2-(N-propylamino)tetralin; EC50, median effective concentration; GTP, guanine 5′-triphosphate; NMDG, N-methyl D-glucamine; (−)-3-PPP, S-(−)-3-(3-hydroxyphenyl)-N-propylpiperidine hydrochloride; UH-232, cis-(+)-5-methoxy-1-methyl-2-(di-N-propylamino)tetralin.