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DOI: 10.1055/s-0031-1298174
© Georg Thieme Verlag KG Stuttgart · New York
GABAA Receptor Modulators from the Chinese Herbal Drug Junci Medulla – The Pith of Juncus effusus
Publication History
received September 22, 2011
revised December 9, 2011
accepted December 18, 2011
Publication Date:
23 January 2012 (online)
![](https://www.thieme-connect.de/media/plantamedica/201205/lookinside/thumbnails/10.1055-s-0031-1298174-1.jpg)
Abstract
The gamma-amino butyric acid (GABA) type A (GABAA) receptor represents a crucial target for clinical agents in the treatment of anxiety and insomnia. Using the two-microelectrode voltage clamp technique on recombinant α 1 β 2 γ 2S GABAA receptors, effusol (1) and dehydroeffusol (2) were isolated in a bioactivity-guided approach from the pith of Juncus effusus L. Both compounds concentration-dependently enhanced GABA induced chloride currents (IGABA) by a maximum 188 ± 20 (1) and 239 ± 18 % (2), independent of the benzodiazepine (BZ) binding site. This activity on the GABAA receptor may explain the traditional use of J. effusus as a sedative and anxiolytic agent in Chinese medicine.
Key words
Juncus effusus L. (Juncaceae) - GABA(A) receptor - voltage clamp - positive allosteric modulation - dehydroeffusol - effusol
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