Tetramethoxyluteolin
Methylated luteolin-analog flavone, a potent human mast cell inhibitor and preclinical neuroprotective candidate.
Pharmacology
Contents
WHAT IS TETRAMETHOXYLUTEOLIN?
Detailed overview
Tetramethoxyluteolin (methlut, methoxyluteolin) is a synthetic, four-fold methoxylated analog of the natural flavone luteolin, developed by Theoharis Theoharides and colleagues at Tufts University. The methoxy groups make it more lipid-soluble and slow its metabolism, so it is a more potent mast cell inhibitor than luteolin itself or cromolyn. In cell and animal models it suppresses the release of inflammatory mediators (histamine, TNF, IL-1β, chemokines) from human mast cells by blocking NF-κB, MAPK and mTOR signaling, and it dampens microglial activation, pointing to neuroprotective and anti-neuroinflammatory potential. Human clinical data are essentially absent: it is an experimental compound that has not been approved as a medicine.
Mechanism
Mast cell inhibition via NF-κB / MAPK / mTOR
Evidence
Preclinical (cell and animal, no human trials)
Legal status
Experimental compound / research flavonoid
Receptor profile
- Human mast cellsStrong
- NF-κB / MAPK inflammatory signalingModerate
- mTOR (microglia)Moderate
- Oxidative stressWeak
Safety
Side effects, stop signs, contraindications
Side effects · 5
- Very limited human safety data: an experimental compound with no established medical use
- Lipid-soluble flavone: may cause GI discomfort on an empty stomach, best taken with food
- Theoretical additive effect with other flavonoids or anti-inflammatory agents
- Long-term safety in humans is not characterized
- As a research-grade preparation, purity and quality can vary
Contraindications · 4
- Pregnancy and breastfeeding: safety not established, avoid
- Not a substitute for prescribed treatment of allergic or inflammatory disease
- Theoretical interaction with CYP-metabolized drugs, as flavones can modulate CYP enzymes
- Avoid in case of known flavone or flavonoid hypersensitivity
Related Nootropics
Same therapeutic category
Studies
Related research and clinical findings
The novel flavone tetramethoxyluteolin is a potent inhibitor of human mast cells
Weng Z, Patel AB, Panagiotidou S, Theoharides TC
Neurotensin stimulates sortilin and mTOR in human microglia inhibitable by methoxyluteolin, a potential therapeutic target for autism
Tsilioni I, Patel AB, Pantazopoulos H, Berretta S, Conti P, Leeman SE, Theoharides TC
Methoxyluteolin Inhibits Neuropeptide-stimulated Proinflammatory Mediator Release via mTOR Activation from Human Mast Cells
Patel AB, Theoharides TC
Substance P and IL-33 administered together stimulate a marked secretion of IL-1β from human mast cells, inhibited by methoxyluteolin
Taracanova A, Alevizos M, Karagkouni A, Weng Z, Norwitz E, Conti P, Leeman SE, Theoharides TC
IL-33 stimulates human mast cell release of CCL5 and CCL2 via MAPK and NF-κB, inhibited by methoxyluteolin
Taracanova A, Tsilioni I, Conti P, Norwitz ER, Leeman SE, Theoharides TC
FAQ
FAQ
Methylated luteolin-analog flavone, a potent human mast cell inhibitor and preclinical neuroprotective candidate.
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Structure & chemistry
The information here is strictly for educational and scientific purposes. It does not replace medical advice or clinical consultation, and it does not encourage illegal substance or pharmaceutical use. Data is sourced. When in doubt, consult your doctor.