Supplements
Flavonoids inhibit MCT1-mediated transport of GHB, reducing sleep time in rats
In vitro, flavonoids such as luteolin, morin, and phloretin inhibited MCT1-mediated uptake of GHB in rat MCT1-transfected cells, with IC50 values of 0.41, 6.41, and 2.57 μM, respectively. In rats, intravenous luteolin (10 mg/kg) increased renal and total clearance of GHB and significantly decreased sleep time from 165 ± 10 min to 121 ± 5 min after a 1000 mg/kg GHB dose.
Evidence Score
Evidence Score26/100
Human RCT
Meta-analysis
Mechanism
Safety
Confidencelow
Study Evidence
Study 1. Flavonoids modulate monocarboxylate transporter-1-mediated transport of gamma-hydroxybutyrate in vitro and in vivo.
observationalWang Q, Morris ME · Drug metabolism and disposition: the biological fate of chemicals (2007)
Participants: N/A
Duration: Acute (single dose)
Intervention: Intravenous administration of luteolin (10 mg/kg) with or without GHB (1000 mg/kg) in rats
Outcome: Sleep time, renal clearance, total clearance of GHB
Effect Size: Sleep time reduction: 44 minutes (121 ± 5 vs 165 ± 10 min)
Population: Male Sprague-Dawley rats
Result:
Mechanism Graph
Flavonoids bind to MCT1 transporter
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Competitive inhibition of GHB uptake at MCT1
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Reduced renal reabsorption of GHB
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Increased GHB clearance and decreased sleep time
Limitations
- ⚠Animal model (rats) may not directly translate to human physiology
- ⚠Only one flavonoid (luteolin) tested in vivo; effects of other flavonoids not confirmed in living animals
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References
- 1.Wang Q, Morris ME. "Flavonoids modulate monocarboxylate transporter-1-mediated transport of gamma-hydroxybutyrate in vitro and in vivo.." Drug metabolism and disposition: the biological fate of chemicals, 2007. PMID: 17108059 DOI: 10.1124/dmd.106.012369
Disclaimer: This content is for educational purposes only and is not medical advice. Evidence scores reflect the quality and quantity of available research, not clinical recommendations. Always consult a healthcare professional before starting any supplement or intervention.