Tier 4 — mechanistic

Flavonoid modulation of ionic currents mediated by GABA(A) and GABA(C) receptors

Juan D. Goutman, Maximiliano D. Waxemberg, Francisco Doñate-Oliver, Pablo E. Pomata, Daniel J. Calvo
European Journal of Pharmacology 2003 461(2-3):79-87

Bibliography

PubMed
PMID 12586201
DOI
10.1016/S0014-2999(03)01309-8
Funding
Not reported in the indexed record reviewed.
Competing interests
Not reported in the indexed record reviewed.

Study snapshot

DesignIn vitro electrophysiology study
ModelGABA(A) and GABA(C) receptors expressed in Xenopus laevis oocytes
SampleElectrophysiological experiments; biological replicate count was not reported in the PubMed abstract.
InterventionApigenin and other natural/synthetic flavonoids tested against GABA-gated ionic currents
DurationAcute in vitro exposure
EndpointsGABA(A)-mediated ionic currents; GABA(C)-mediated ionic currents; Flumazenil sensitivity; Flavonoid concentration-response effects

What the study showed, in plain terms

This electrophysiology study tested whether apigenin and related flavonoids directly modulate ionotropic GABA receptor currents.

Key findings

In the tested receptor systems, apigenin inhibited rather than potentiated GABA(A) and GABA(C) currents in the micromolar range, and its GABA(A) effect was insensitive to flumazenil. This argues against a simplistic claim that apigenin merely boosts GABA-A signaling like a benzodiazepine.

What this study can and cannot tell us

The receptors were expressed in Xenopus oocytes, so these findings do not directly predict brain exposure, whole-animal behavior, human sleep outcomes or effects at typical oral supplement concentrations.

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Dr. Khaled Mahmoud, MBBChCritical Care Medicine, Longevity Science & Editorial Direction Dr. Amr Yasser, PhDCardiometabolic, Musculoskeletal, Gut & Bioavailability Dr. Abdulla Mostafa, PhDCellular Senescence, Neurological, Mitochondrial & Brain-Ageing Biology