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

Milanos S, Elsharif S, Janzen D, Büttner A, Villmann C (2017)

Publication Status: Published

Publication Type: Journal article

Publication year: 2017

Journal

Frontiers in Chemistry Frontiers

Publisher: FRONTIERS MEDIA SA

Book Volume: 5

DOI: 10.3389/fchem.2017.00046

Abstract

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.

Authors with CRIS profile

Sinem Milanos Lehrstuhl für Aroma- und Geruchsforschung Shaimaa Elsharif
Andrea Büttner

Involved external institutions

Julius-Maximilians-Universität Würzburg DE Germany (DE)

How to cite

APA:

Milanos, S., Elsharif, S., Janzen, D., Büttner, A., & Villmann, C. (2017). Metabolic Products of Linalool and Modulation of GABA(A) Receptors. Frontiers in Chemistry, 5. https://dx.doi.org/10.3389/fchem.2017.00046

MLA:

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

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