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.
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Flavonoids inhibit MCT1-mediated transport of GHB, reducing sleep time in rats The current body of evidence comprises 1 study. EvidenceHub rates the overall confidence at 26/100 (low).
The Claim
Flavonoids inhibit MCT1-mediated transport of GHB, reducing sleep time in rats
This conclusion is most relevant to: Rats (in vivo); rat MCT1-transfected MDA-MB231 cells (in vitro).
What the Research Shows
The conclusion draws on 1 linked study. Highlights from the cited literature:
- ▸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) —
How It Works
The proposed biological pathway:
- ▸Flavonoids bind to MCT1 transporter
- ▸Competitive inhibition of GHB uptake at MCT1
- ▸Reduced renal reabsorption of GHB
- ▸Increased GHB clearance and decreased sleep time
Who Might Benefit
Evidence fit by population:
- ▸Rats (in vivo); rat MCT1-transfected MDA-MB231 cells (in vitro)
Recommended Dose
Luteolin 10 mg/kg i.v.; GHB 1000 mg/kg i.v.
Limitations & Caveats
Important context when interpreting this evidence:
- ▸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
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