Receptor profiles of ATC0065 and ATC0175
Affinity for each receptor was evaluated by receptor binding assays for each receptor, as described under Materials and Methods. Antagonistic activity was evaluated by [35S]GTPγS binding (MCHR1) or [Ca2+]i (MCHR2). Data represents mean ± S.E. obtained from three to five separate experiments, each done in duplicate. n is shown in parentheses.
MCHR1 | MCHR2 Antagonist Activity | 5-HT2B Affinity | 5-HT1A Affinity | |||
|---|---|---|---|---|---|---|
| Affinity | Antagonist Activity | |||||
| IC50 (nM) | ||||||
| ATC0065 | 15.7 ± 1.95 (4) | 21.4 ± 1.57 (3) | 1510 ± 140 (3) | 266 ± 91.8 (3) | 62.9 ± 11.8 (5) | |
| ATC0175 | 7.23 ± 0.59 (3) | 13.5 ± 0.78 (3) | >10,000 (3) | 9.66 ± 1.58 (5) | 16.9 ± 1.56 (5) | |