Effects of Valeriana Officinalis Extracts on [3H]Flunitrazepam Binding, Synaptosomal [3H]GABA Uptake, and Hippocampal [3H]GABA Release

Neurochemical Research - 1999
José G. Ortiz1,2, Jennifer Nieves-Natal2,1, Pedro Chavez3,4
1School of Pharmacy, San Juan, Puerto Rico
2Department of Pharmacology and Toxicology, University of Puerto Rico School of Medicine, Puerto Rico
3Dept. of Medicinal Chemistry and Pharmacognosy, Midwestern University-Glendale College of Pharmacy, Glendale
4Center for Molecular and Behavioral Neuroscience, Universidad Central del Caribe, Bayamón, Puerto Rico

Tóm tắt

Extracts of Valeriana officinalis have been used in folkloric medicine for its sedative, hypnotic, tranquilizer and anticonvulsant effects, and may interact with γ-aminobutyric acid (GABA) and/or benzodiazepine sites. At low concentrations, valerian extracts enhance [3H]flunitrazepam binding (EC50 4.13 × 10−10 mg/ml). However, this increased [3H]flunitrazepam binding is replaced by an inhibition at higher concentrations (IC50 of 4.82 × 10−1 mg/ml). These results are consistent with the presence of at least two different biological activities interacting with [3H]flunitrazepam binding sites. Valerian extracts also potentiate K+ or veratridine-stimulated release of radioactivity from hippocampal slices preloaded with [3H]GABA. Finally, inhibition of synaptosomal [3H]GABA uptake by valerian extracts also displays a biphasic interaction with guvacine. The results confirm that valerian extracts have effects on GABAA receptors, but can also interact at other presynaptic components of GABAergic neurons.

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Tài liệu tham khảo

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