Endocannabinoid transport revisited.

Nicolussi, Simon; Gertsch, Jürg (2015). Endocannabinoid transport revisited. In: Litwack, Gerald (ed.) Vitamins and Hormones. Hormones and Transport Systems: Vol. 98 (pp. 441-485). Elsevier Inc. 10.1016/bs.vh.2014.12.011

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Endocannabinoids are arachidonic acid-derived endogenous lipids that activate the endocannabinoid system which plays a major role in health and disease. The primary endocannabinoids are anandamide (AEA, N-arachidonoylethanolamine) and 2-arachidonoyl glycerol. While their biosynthesis and metabolism have been studied in detail, it remains unclear how endocannabinoids are transported across the cell membrane. In this review, we critically discuss the different models of endocannabinoid trafficking, focusing on AEA cellular uptake which is best studied. The evolution of the current knowledge obtained with different AEA transport inhibitors is reviewed and the confusions caused by the lack of their specificity discussed. A comparative summary of the most important AEA uptake inhibitors and the studies involving their use is provided. Based on a comprehensive literature analysis, we propose a model of facilitated AEA membrane transport followed by intracellular shuttling and sequestration. We conclude that novel and more specific probes will be essential to identify the missing targets involved in endocannabinoid membrane transport.

Item Type:

Book Section (Book Chapter)

Division/Institute:

04 Faculty of Medicine > Pre-clinic Human Medicine > Institute of Biochemistry and Molecular Medicine

Graduate School:

Graduate School for Cellular and Biomedical Sciences (GCB)

UniBE Contributor:

Nicolussi, Simon and Gertsch, Jürg

Subjects:

500 Science > 570 Life sciences; biology
600 Technology > 610 Medicine & health

ISSN:

0083-6729

ISBN:

978-0-12-803008-0

Series:

Hormones and Transport Systems

Publisher:

Elsevier Inc.

Language:

English

Submitter:

Kevin Marc Rupp

Date Deposited:

19 May 2015 10:00

Last Modified:

28 Oct 2019 04:16

Publisher DOI:

10.1016/bs.vh.2014.12.011

PubMed ID:

25817877

Uncontrolled Keywords:

2-AG; Anandamide; Endocannabinoid system; Endocannabinoid uptake and transport; Endocannabinoid uptake inhibitor; FAAH; Membrane transporter

BORIS DOI:

10.7892/boris.68420

URI:

https://boris.unibe.ch/id/eprint/68420

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