← Compounds

Orexin A

peptide · headlineResearch use only

Binds 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: mg
    low dose: 1
    frequency: 1x daily in the morning or before demanding cognitive activity
    high dose: 5
    standard dose: 2.5
    administration 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

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.