Kyotorphin
Kyotorphin (Tyr-Arg) is a fascinating endogenous neuro-dipeptide first isolated from mammalian brain tissue. Operating as a master modulator of pain and neural preservation, it commands intense interest in advanced neurology. It is heavily evaluated for its profound non-opioid analgesic properties, its ability to forcibly halt neurodegenerative disease states, and its aggressive anti-amyloid actions in Alzheimer’s models.
Quick Stats
Scientific Data
Mechanism of Action
Kyotorphin (L-Tyrosyl-L-Arginine) is a naturally occurring neuroactive dipeptide isolated from the bovine brain in 1979 in Kyoto, Japan. It functions as an endogenous analgesic neurotransmitter/neuromodulator.
Unlike opioid peptides (endorphins/enkephalins) which bind directly to opioid receptors, Kyotorphin exerts its profound pain-relieving effects (4-5x stronger than met-enkephalin) indirectly. It stimulates the regional release of endogenous enkephalins and modulates synaptic calcium channels. Because it does not directly agonize opioid receptors, it does not produce typical opioid tolerance or physical dependence, making it a highly investigated molecule in pain biology.
Source: PMID: 3427544
Background & History
Kyotorphin was discovered in 1979 by Hiroshi Takagi at Kyoto University during a systematic search for endogenous analgesic substances in bovine brain. It was the first non-opioid endogenous analgesic dipeptide identified. Recent decades have expanded interest beyond analgesia to neuroprotection: Kyotorphin derivatives show promise in reducing amyloid-β neurotoxicity and modulating glutamatergic transmission, making it a candidate for Alzheimer disease research.
Research Use Cases
- ✓Endogenous analgesia research
- ✓Neuroprotection research
- ✓Alzheimer disease research
- ✓NMDA receptor modulation
Dosing Protocol
| Typical Dose | 1-10 mg ICV/intranasal (research) |
| Frequency | Per study protocol |
| Half-Life | ~0.3 hours |
| Common Vial Sizes | 5 mg |
Dosing Protocols
Research Only
Body-Weight Dosing Reference
Estimated doses extrapolated from the published research range of 1000–10000 mcg/day (referenced to 70 kg / 154 lb). These are approximations — consult a qualified healthcare provider for personalised guidance.
| Weight | Low Dose | Target Dose | High Dose |
|---|---|---|---|
| 120 lb(54 kg) | 771 mcg | 4243 mcg | 7714 mcg |
| 140 lb(63 kg) | 900 mcg | 4950 mcg | 9000 mcg |
| 160 lb(73 kg) | 1043 mcg | 5736 mcg | 10429 mcg |
| 180 lb(82 kg) | 1171 mcg | 6443 mcg | 11714 mcg |
| 200 lb(91 kg) | 1300 mcg | 7150 mcg | 13000 mcg |
| 220 lb(100 kg) | 1429 mcg | 7857 mcg | 14286 mcg |
| 250 lb(113 kg) | 1614 mcg | 8879 mcg | 16143 mcg |
💉 For exact syringe units based on your vial concentration, use the Kyotorphin Reconstitution Calculator →
Administration
Expected Timeline
Who Is It For?
Endogenous Analgesia
LowImportant mechanistic discovery in neuroscience. Too unstable and BBB-impermeable for standard therapeutic use.
Reconstitution Example
Safety & Considerations
Endogenous molecule. No human clinical dosing protocol exists due to blood-brain barrier permeability issues and rapid enzymatic degradation in plasma.
Regulatory & Legal Status
Not currently on the WADA 2026 Prohibited List. Policies may change — verify before competition.
Research Chemical
US Compounding: Not eligible / not available
⚠️ This information is for educational purposes only and may not reflect the most current regulatory updates. Always verify with official FDA, WADA, and jurisdiction-specific sources before use.
Interactions & Contraindications
Research compound. May potentiate effects of opioid analgesics through enkephalin amplification. Theoretical interaction with NMDA modulators.
Synergies & Common Stacks
Kyotorphin (enkephalin release) + Selank (anxiolytic tuftsin analogue) — both modulate endogenous opioid and enkephalin systems through complementary mechanisms.
Kyotorphin + Semax for dual neuroprotective approach: Kyotorphin via enkephalin/NMDA modulation, Semax via BDNF expression.
Dosing Quick Reference
Frequently Asked Questions
Is Kyotorphin an opioid?▼
References
- Takagi H et al. “"Isolation and structure of a new analgesic dipeptide (kyotorphin) from bovine brain".” Nature (1979). PMID: 512406
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