Metabolic Products of Linalool and Modulation of GABA(A) Receptors

Journal article

Publication Details

Author(s): Milanos S, Elsharif S, Janzen D, Büttner AK, Villmann C
Journal: Frontiers in Chemistry
Publication year: 2017
Volume: 5
ISSN: 2296-2646


Terpenoids are major subcomponents in aroma substances which harbor sedative physiological potential. We have demonstrated that various monoterpenoids such as the acyclic linalool enhance GABAergic currents in an allosteric manner in vitro upon overexpression of inhibitory alpha 1 beta 2 GABA(A) receptors in various expression systems. However, in plants or humans, i.e., following intake via inhalation or ingestion, linalool undergoes metabolic modifications including oxygenation and acetylation, which may affect the modulatory efficacy of the generated linalool derivatives. Here, we analyzed the modulatory potential of linalool derivatives at alpha 1 beta 2 gamma 2 GABA(A) receptors upon transient overexpression. Following receptor expression control, electrophysiological recordings in a whole cell configuration were used to determine the chloride influx upon co-application of GABA EC10-30 together with the modulatory substance. Our results show that only oxygenated linaloolmetabolites at carbon 8 positively affect GABAergic currents whereas derivatives hydroxylated or carboxylated at carbon 8 were rather ineffective. Acetylated linalool derivatives resulted in non-significant changes of GABAergic currents. We can conclude that metabolism of linalool reduces its positive allosteric potential at GABA(A) receptors compared to the significant potentiation effects of the parent molecule linalool itself.

FAU Authors / FAU Editors

Büttner, Andrea Prof. Dr.
Professur für Aromaforschung
Elsharif, Shaimaa
Professur für Aromaforschung
Milanos, Sinem
Lehrstuhl für Aroma- und Geruchsforschung

External institutions with authors

Julius-Maximilians-Universität Würzburg

How to cite

Milanos, S., Elsharif, S., Janzen, D., Büttner, A.K., & Villmann, C. (2017). Metabolic Products of Linalool and Modulation of GABA(A) Receptors. Frontiers in Chemistry, 5.

Milanos, Sinem, et al. "Metabolic Products of Linalool and Modulation of GABA(A) Receptors." Frontiers in Chemistry 5 (2017).


Last updated on 2018-23-08 at 10:08