ArticleEuropean journal of pharmacology2011
Insights into structure-activity relationship of GABAA receptor modulating coumarins and furanocoumarins.
Article in European journal of pharmacology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 46 citations in OpenAlex.
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- Influence of Umbelliferone on the Anticonvulsant and Neuroprotective Activity of Selected Antiepileptic Drugs: An In Vivo and In Vitro Study.International journal of molecular sciences · 2022Article
- Comparative Antiseizure Analysis of Diverse Natural Coumarin Derivatives in Zebrafish.International journal of molecular sciences · 2021Article
- Oxypeucedanin: Chemotaxonomy, Isolation, and Bioactivities.Plants (Basel, Switzerland) · 2021Review
- Coumarins fromInternational journal of molecular sciences · 2021Article
- The Protective Effect of Auraptene Against Oxidative Stress and Pentylenetetrazol-Induced Chemical Kindling in Mice.Iranian journal of pharmaceutical research : IJPR · 2019Article
- Structure-Dependent Activity of Natural GABA(A) Receptor Modulators.Molecules (Basel, Switzerland) · 2018Review
- The Effect of 4-hydroxybenzaldehyde on the γ-aminobutyric Acid Type A Receptor.The Malaysian journal of medical sciences : MJMS · 2017Article
- In vivo modulation of the behavioral effects of nicotine by the coumarins xanthotoxin, bergapten, and umbelliferone.Psychopharmacology · 2016Article
- Osthole: A Review on Its Bioactivities, Pharmacological Properties, and Potential as Alternative Medicine.Evidence-based complementary and alternative medicine : eCAM · 2015Review
- Coumarin compounds of Biebersteinia multifida roots show potential anxiolytic effects in mice.Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences · 2013Article
- GABAA receptor modulation by piperine and a non-TRPV1 activating derivative.Biochemical pharmacology · 2013Article
- Imperatorin-pharmacological meaning and analytical clues: profound investigation.Phytochemistry reviews : proceedings of the Phytochemical Society of EuropeReview
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
The coumarins imperatorin and osthole are known to exert anticonvulsant activity. We have therefore analyzed the modulation of GABA-induced chloride currents (I(GABA)) by a selection of 18 coumarin derivatives on recombinant α(1)β(2)γ(2S) GABA(A) receptors expressed in Xenopus laevis oocytes by means of the two-microelectrode voltage clamp technique. Osthole (EC(50)=14 ± 1 μM) and oxypeucedanin (EC(50)=25 ± 8 μM) displayed the highest efficiency with I(GABA) potentiation of 116 ± 4 % and 547 ± 56 %, respectively. I(GABA) enhancement by osthole and oxypeucedanin was not inhibited by flumazenil (1 μM) indicating an interaction with a binding site distinct from the benzodiazepine binding site. In general, prenyl residues are essential for the positive modulatory activity, while longer side chains or bulkier residues (e.g. geranyl residues) diminish I(GABA) modulation. Generation of a binary classification tree revealed the importance of polarisability, which is sufficient to distinguish actives from inactives. A 4-point pharmacophore model based on oxypeucedanin - comprising three hydrophobic and one aromatic feature - identified 6 out of 7 actives as hits. In summary, (oxy-)prenylated coumarin derivatives from natural origin represent new GABA(A) receptor modulators.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.