Abstract
The gamma-amino butyric acid (GABA) type A (GABA(A)) receptor represents a crucial target for clinical agents in the treatment of anxiety and insomnia. Using the two-microelectrode voltage clamp technique on recombinant α₁β₂γ(2S) GABA (A) 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 (I(GABA)) by a maximum 188 ± 20 (1) and 239 ± 18 % (2), independent of the benzodiazepine (BZ) binding site. This activity on the GABA (A) receptor may explain the traditional use of J. effusus as a sedative and anxiolytic agent in Chinese medicine.
© Georg Thieme Verlag KG Stuttgart · New York.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-Anxiety Agents / chemistry
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Anti-Anxiety Agents / isolation & purification
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Anti-Anxiety Agents / pharmacology*
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Dose-Response Relationship, Drug
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Drugs, Chinese Herbal / chemistry
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Drugs, Chinese Herbal / isolation & purification
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Drugs, Chinese Herbal / pharmacology*
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GABA Modulators / chemistry
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GABA Modulators / isolation & purification
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GABA Modulators / pharmacology*
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Hypnotics and Sedatives / chemistry
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Hypnotics and Sedatives / isolation & purification
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Hypnotics and Sedatives / pharmacology*
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Magnoliopsida / chemistry*
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Molecular Structure
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Patch-Clamp Techniques
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Phenanthrenes / chemistry
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Phenanthrenes / isolation & purification
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Phenanthrenes / pharmacology
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Phenols / chemistry
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Phenols / isolation & purification
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Phenols / pharmacology
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Receptors, GABA-A / drug effects*
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Receptors, GABA-A / metabolism
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Recombinant Proteins
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gamma-Aminobutyric Acid / metabolism
Substances
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Anti-Anxiety Agents
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Drugs, Chinese Herbal
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GABA Modulators
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Hypnotics and Sedatives
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Phenanthrenes
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Phenols
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Receptors, GABA-A
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Recombinant Proteins
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dehydroeffusol
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gamma-Aminobutyric Acid