OX1 antagonist
Orexin-1 receptor antagonist
OX1 antagonist — mechanism card
- ↓ reward/arousal signaling
- Weakly hypnotic alone — the sleep of dual orexin antagonists comes mainly from OX2 blockade
- May ↓ drug-seeking (preclinical)
- depression-like behavior in rats
Drugs with this mechanism (3)
- Daridorexant — Dual orexin antagonist hypnotic with a short half-life for less next-day effect.
- Lemborexant — Dual orexin antagonist hypnotic.
- Suvorexant — Dual orexin antagonist for sleep-onset and sleep-maintenance insomnia.
Self-check
- Why is OX1 blockade only weakly hypnotic alone?
Dual-antagonist sleep effects come mainly from OX2 blockade. - How established is reduced drug-seeking with OX1 blockade here?
It may occur; evidence is preclinical.
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