title: GABA(A) receptor modulators from the Chinese herbal drug Junci Medulla--the pith of Juncus effusus.
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.
authors.affiliation: Department of Pharmacognosy, University of Vienna, Vienna, Austria.
authors.forename: Judith
authors.initials: J
authors.lastname: Singhuber
authors.forename: Igor
authors.initials: I
authors.lastname: Baburin
authors.forename: Sophia
authors.initials: S
authors.lastname: Khom
authors.forename: Martin
authors.initials: M
authors.lastname: Zehl
authors.forename: Ernst
authors.initials: E
authors.lastname: Urban
authors.forename: Steffen
authors.initials: S
authors.lastname: Hering
authors.forename: Brigitte
authors.initials: B
authors.lastname: Kopp
mesh_terms: D014151:Anti-Anxiety Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D018757:GABA Modulators / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D006993:Hypnotics and Sedatives / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D019684:Magnoliopsida / Q000737:chemistry*; D015394:Molecular Structure; D018408:Patch-Clamp Techniques; D010616:Phenanthrenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D010636:Phenols / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D011963:Receptors, GABA-A / Q000187:drug effects* / Q000378:metabolism; D011994:Recombinant Proteins; D005680:gamma-Aminobutyric Acid / Q000378:metabolism
chemical_list: D014151:Anti-Anxiety Agents; D004365:Drugs, Chinese Herbal; D018757:GABA Modulators; D006993:Hypnotics and Sedatives; D010616:Phenanthrenes; D010636:Phenols; D011963:Receptors, GABA-A; D011994:Recombinant Proteins; C573784:dehydroeffusol; D005680:gamma-Aminobutyric Acid