Endocannabinoid Transport Revisited

Nicolussi, Simon; Gertsch, Jürg

doi:10.1016/bs.vh.2014.12.011

Cited by 91 publications

(98 citation statements)

References 150 publications

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“…Though still incomplete, the limited available data suggest that a putative transporter controls the anandamide trafficking (Cravatt et al, 2001;Kathuria et al, 2003;Makriyannis, 2014;Fezza et al, 2014;Batista et al, 2014;Nicolussi and Gertsch, 2015). Regarding the role of AMT in sleep modulation, this issue has been poorly studied.…”

Section: Discussionmentioning

confidence: 99%

“…An additional actor of the endocannabinoid system includes the anandamide membrane transporter (AMT) which displays a key role in modulating anandamide's biological functions (Chicca et al, 2012;Fowler, 2013;Khasabova et al, 2013;Leung et al, 2013;Nicolussi and Gertsch, 2015). The available evidence indicates that injections of blocker of AMT known as VDM-11 promote sleep in rats (Murillo-Rodrı´guez et al, 2008.…”

Section: Introductionmentioning

confidence: 99%

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Revealing the role of the endocannabinoid system modulators, SR141716A, URB597 and VDM-11, in sleep homeostasis

et al. 2016

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Abstract-The endocannabinoid system comprises receptors (CB 1 and CB 2 cannabinoid receptors), enzymes (Fatty Acid Amide Hydrolase [FAAH], which synthesizes the endocannabinoid anandamide), as well as the anandamide membrane transporter (AMT). Importantly, previous experiments have demonstrated that the endocannabinoid system modulates multiple neurobiological functions, including sleep. For instance, SR141716A (the CB 1 cannabinoid receptor antagonist) as well as URB597 (the FAAH inhibitor) increase waking in rats whereas VDM-11 (the blocker of the AMT) enhances sleep in rodents. However, no further evidence is available regarding the neurobiological role of the endocannabinoid system in the homeostatic control of sleep. Therefore, the aim of the current experiment was to test if SR141716A, URB597 or VDM-11 would modulate the sleep rebound after sleep deprivation. Thus, these compounds were systemically injected (5, 10, 20 mg/kg; ip; separately each one) into rats after prolonged waking. We found that SR141716A and URB597 blocked in dose-dependent fashion the sleep rebound whereas animals treated with VDM-11 displayed sleep rebound during the recovery period. Complementary, injection after sleep deprivation of either SR141716A or URB597 enhanced dose-dependently the extracellular levels of dopamine (DA), norepinephrine (NE), epinephrine (EP), serotonin (5-HT), as well as adenosine (AD) while VDM-11 caused a decline in contents of these molecules. These findings suggest that SR141716A or URB597 behave as a potent stimulants since they suppressed the sleep recovery period after prolonged waking. It can be concluded that elements of the endocannabinoid system, such as the CB 1 cannabinoid receptor, FAAH and AMT, modulate the sleep homeostasis after prolonged waking. Ó

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Revealing the role of the endocannabinoid system modulators, SR141716A, URB597 and VDM-11, in sleep homeostasis

et al. 2016

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“…A FLAT transporter (fatty acid amide hydrolase-like anandamide transporter) has been discovered recently for intracellular transport of AEA [63], but a study published one year later contradicts its putative role [64]. It is thus too soon to conclude clearly on this point [49,55]. In addition, recent studies revealed that the preferred target of AEA in the brain may be postsynaptic TRPV1 (transient receptor potential vallinoid 1) channels and not necessarily presynaptic receptors.…”

Section: Aea Metabolismmentioning

confidence: 99%

“…2-AG is thus a retrograde messenger that is released from the post-synapse into the synaptic cleft. The question of an active transporter for 2-AG has been densely investigated but up to now, there is no identified transporter for 2-AG [55]. The most likely hypothesis at present is that DAGL enzyme is responsible for release of 2-AG in the synaptic cleft.…”

Section: -Ag Metabolismmentioning

confidence: 99%

Dietary Omega-6/Omega-3 and Endocannabinoids: Implications for Brain Health and Diseases

Bosch‐Bouju¹,

Layé²

2016

Cannabinoids in Health and Disease

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Omega-3 (ω-3) and omega-6 (ω-6) are polyunsaturated fatty acids (PUFAs) that play critical role in human health and have to be provided by food. In the brain, PUFAs are also precursors of endocannabinoids. The aim of this chapter is to review the existing literature on how dietary PUFAs impact on the endocannabinoid system in the brain and what are the consequences for brain function and dysfunction. In this chapter, we will first describe how PUFAs enter the brain, what are their metabolism processes and roles in brain function. We will describe the pathways from PUFAs to endocannabinoid production. Then, we will review the literature on how dietary ω-6/ω-3 ratio impacts the endocannabinoid system, in terms of endocannabinoid levels, proteins and endocannabinoid-dependent synaptic plasticity. In the next part, we will describe what we know about the interactions between PUFAs and endocannabinoids in neurological and neuropsychiatric disorders. Finally, we will conclude on the possible implications of the interactions between dietary PUFAs and endocannabinoids in the normal and pathological brain. In particular, we will discuss how dietary PUFAs, as homeostatic regulators of endocannabinoids, can constitute interesting therapeutic strategies for the prevention and/or treatment of neurological disorders with endocannabinoids impairment.

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“…Here, we describe a radiosubstrate-based assay using arachidonoyl[1-3 H]ethanolamine or arachidonoyl [1,2, H]glycerol to measure the cellular endocannabinoid uptake in a three-phase assay with human U937 cells. …”

mentioning

confidence: 99%