Table 4.
CNS Receptor Binding Profile.
Receptor | Radioligand Binding Assay IC50 (nM)1 | ||
---|---|---|---|
8 | 17d | 17e | |
D1 | 44 | 1157 | 1,403 |
D2 | 541 | 993 | >10,000 |
D3 | 29 | 235 | 2,307 |
D4 | 416 | >10,000 | >10,000 |
D5 | 70 | 1,477 | 1,336 |
5-HT1A | 670 | 1,242 | >10,000 |
5-HT1B | 1,210 | >10,000 | >10,000 |
5-HT1E | >10,000 | >10,000 | >10,000 |
5-HT2A | 11 | 183 | 325 |
5-HT2B | 112 | 243 | 347 |
5-HT2C | 63 | 127 | 464 |
5-HT3 | 581 | >10,000 | >10,000 |
5-HT5a | 1,795 | >10,000 | >10,000 |
5-HT6 | 235 | 1,102 | 2,470 |
Compounds with <50% inhibition at 10 μM are reported as >10,000 nM.