Baicalein
Skullcap flavone (5,6,7-trihydroxyflavone), a GABA-A modulator with antioxidant and calming profile, preclinical data only.
Pharmacology
Contents
WHAT IS BAICALEIN?
Detailed overview
Baicalein (5,6,7-trihydroxyflavone) is a flavone from the root of Baikal skullcap (Scutellaria baicalensis) and related skullcap species, long used in traditional Chinese medicine. Its three adjacent hydroxyl groups give it strong metal-chelating and free-radical-scavenging antioxidant activity, and the compound also acts as a positive allosteric modulator of the GABA-A receptor, producing mild anxiolytic and calming effects in animal models. It inhibits lipoxygenase and other inflammatory enzymes and shows neuroprotective activity in numerous rodent and fish models. There is no human clinical evidence for a nootropic/anxiolytic use: the effects are mainly preclinical, and poor oral bioavailability leaves the human assessment largely unexplored.
Mechanism
GABA-A PAM + antioxidant / LOX-inhibiting flavone
Evidence
Preclinical only (no human RCT)
Legal status
Herbal extract / dietary-supplement ingredient
Receptor profile
- Antioxidant / oxidative-stress reductionStrong
- GABA-A receptors (benzodiazepine site)Moderate
- Lipoxygenase (12/15-LOX) inhibitionModerate
- Serotonin / dopamine signalingWeak
Safety
Side effects, stop signs, contraindications
Side effects · 6
- No established human dosing or safety profile: evidence comes largely from animal and cell studies
- May inhibit drug-metabolizing enzymes (CYP3A4, CYP1A2, UGT), altering blood levels of other agents
- May affect blood-clotting and platelet-aggregation pathways (theoretical bleeding risk)
- Poor oral bioavailability due to rapid glucuronidation, so effects vary between individuals
- Theoretical sedation or drowsiness at higher doses from GABAergic modulation
- Possible gastrointestinal upset with skullcap (Scutellaria) extracts
Contraindications · 4
- Pregnancy and breastfeeding: safety not established, avoid
- Anticoagulant or antiplatelet therapy, or before planned surgery: possible bleeding risk
- Concurrent use of CYP3A4/CYP1A2-metabolized drugs: interaction risk
- Not an approved medicine; herbal/research compound without standardized dosing, medical consultation advised
Related Nootropics
Same therapeutic category
Studies
Related research and clinical findings
Baicalein exerts anxiolytic and antinociceptive effects in a mouse model of posttraumatic stress disorder
Baicalein prevents stress-induced anxiety behaviors in zebrafish model
Brain Uptake of Bioactive Flavones in Scutellariae Radix and Its Relationship to Anxiolytic Effect in Mice
Baicalein reduces beta-amyloid and promotes nonamyloidogenic amyloid precursor protein processing in an Alzheimer's disease transgenic mouse model
Assessment of the treatment effect of baicalein on a model of Parkinsonian tremor and elucidation of the mechanism
FAQ
FAQ
Skullcap flavone (5,6,7-trihydroxyflavone), a GABA-A modulator with antioxidant and calming profile, preclinical data only.
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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.