Table 2.
Summary of orexin receptor antagonists.
| Name | Affinity (Ki, nM) | Possible applications | |||
|---|---|---|---|---|---|
| OX1R | OX2R | ||||
| SINGLE OREXIN | SELECTIVITY | ||||
| RECEPTOR ANTAGONIST | |||||
| SB-334867 | 28 | 1704 | OX1R | Withdrawal, substance abuse, obesity, panic disorder | |
| SB-408124 | 22 | 1405 | |||
| SB-674042 | 1.1 | 129 | |||
| ACT-335827 | 6 | 417 (IC50) | |||
| TCS-OX2-29 | – | 7.4 (pKi) | OX2R | Sleep promotion | |
| JNJ-10397049 | 1644 | 6 | |||
| EMPA | 900 | 1.1 | |||
| Antagonist 26 | 6.34 | 7.23 (pKi) | |||
| DUAL OREXIN | FDA PHASE | ||||
| RECEPTOR ANTAGONIST | |||||
| Almorexant | 13 | 8 | III (discontinued) | Treatment of insomnia | |
| SB-649868 | 0.3 | 0.4 | II (completed) | ||
| Suvorexant | 0.6 | 0.4 | III (pending approval) | ||
| MK-6096 | 2.5 | 0.3 | – | – | |
| DORA 30 | 18 | 7 (IC50) | – | Sleep promotion | |