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Flavonoids inhibit MCT1-mediated transport of gamma-hydroxybutyrate, 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 vivo, intravenous luteolin (10 mg/kg) increased renal and total clearance of GHB and significantly reduced sleep time from 165 to 121 minutes in rats given 1000 mg/kg GHB.

Last updated: Aug 25, 2026•0 RCTs•📖 Read as article →

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.

observational

Wang 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:

PubMed: 17108059DOI: 10.1124/dmd.106.012369

Mechanism Graph

Flavonoids (e.g., luteolin) competitively inhibit MCT1 transporter
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Inhibition reduces renal reabsorption of GHB in kidney
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Increased renal and total clearance of GHB
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Result: Decreased GHB brain levels and reduced sleep time

Limitations

  • ⚠Animal study (rats) may not directly translate to humans
  • ⚠Only one flavonoid (luteolin) tested in vivo; others only in vitro
  • ⚠Single dose of GHB and luteolin; dose-response not fully explored

Frequently Asked Questions

What flavonoids were found to inhibit GHB transport?▼

Apigenin, biochanin A, chrysin, diosemin, fisetin, genistein, hesperitin, kaempferol, luteolin, morin, narigenin, phloretin, and quercetin inhibited MCT1-mediated GHB uptake in vitro.

Did luteolin reduce sleep time in rats?▼

Yes, luteolin (10 mg/kg i.v.) significantly decreased sleep time from 165 to 121 minutes after GHB administration.

Are flavonoids substrates for MCT1?▼

No, kaempferol and biochanin A were not taken up via MCT1, suggesting flavonoids are inhibitors but not substrates.

What was the mechanism of inhibition for luteolin?▼

Luteolin competitively inhibited MCT1-mediated GHB transport with an IC50 of 0.41 μM.

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References

  1. 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.