Neurochemical Research

, Volume 24, Issue 11, pp 1373–1378

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

  • José G. Ortiz
  • Jennifer Nieves-Natal
  • Pedro Chavez
Article

DOI: 10.1023/A:1022576405534

Cite this article as:
Ortiz, J.G., Nieves-Natal, J. & Chavez, P. Neurochem Res (1999) 24: 1373. doi:10.1023/A:1022576405534

Abstract

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.

Valeriana [3H]flunitrazepam [3H]GABA uptake [3H]GABA release 

Copyright information

© Plenum Publishing Corporation 1999

Authors and Affiliations

  • José G. Ortiz
    • 1
    • 3
  • Jennifer Nieves-Natal
    • 1
    • 3
  • Pedro Chavez
    • 2
    • 4
  1. 1.Department of Pharmacology and ToxicologyUniversity of Puerto Rico School of MedicinePuerto Rico
  2. 2.Center for Molecular and Behavioral NeuroscienceUniversidad Central del CaribeBayamónPuerto Rico
  3. 3.School of PharmacySan JuanPuerto Rico
  4. 4.Dept. of Medicinal Chemistry and PharmacognosyMidwestern University-Glendale College of PharmacyGlendale

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