← Compounds
Orexin A
peptide · headlineResearch use onlyBinds to orexin receptor 1 (OX1R) and orexin receptor 2 (OX2R) in the brain
Summary
Orexin A is a wake-promoting neuropeptide that modulates sleep, alertness, appetite, and cognitive function. It acts on orexin receptors in the brain and is being researched as a treatment for narcolepsy, fatigue, and age-related cognitive decline. Intranasal delivery allows fast CNS uptake for energizing and neurostimulant effects.
How it works
- Binds to orexin receptor 1 (OX1R) and orexin receptor 2 (OX2R) in the brain
- Activates neurons in the hypothalamus, brainstem, and cortex
- Promotes sustained wakefulness by modulating dopamine, norepinephrine, histamine, and acetylcholine pathways
- Regulates energy homeostasis, feeding, and reward signaling
Dosing
- unit: mglow dose: 1frequency: 1x daily in the morning or before demanding cognitive activityhigh dose: 5standard dose: 2.5administration route: Intranasal
Cycling
- Use 1x daily in the morning or pre-task. Cycle 5 days on, 2 days off if used long-term to prevent desensitization.
Side effects
common: ["Mild headache","Nasal dryness","Increased heart rate"]
warnings: ["Avoid use in individuals with severe cardiovascular disease or insomnia","May exacerbate anxiety or restlessness in sensitive users"]
long term: ["Limited long-term human data; use cautiously in chronic regimens"]
Chemistry & PK
sequence: NH2-CDSPCSVGPGVVGPGVNGVGNGRKSGSKSQTQTQTQTQTQTQTQTQTV-COOH
half life: 15–30 minutes systemically; CNS effects last longer
degradation: Metabolized by peptidases in blood and brain
molecular weight: 3562.1
molecular formula: C146H246N44O42S1
tissue specificity: Targets orexin neurons in hypothalamus, cortex, and limbic regions
Verified citations
2 · PubMed-checked- The neural circuit of orexin (hypocretin): maintaining sleep and wakefulness.mechanismPMID 17299454 ↗
- Narcolepsy - clinical spectrum, aetiopathophysiology, diagnosis and treatment.reviewPMID 31324898 ↗
Used for
Legal / compounding
Research use only
Legal status is a hard gate: non-compoundable or delisted agents cannot be filled and are blocked from protocol export. Keep 503A status current.