Multiple endocannabinoid-mediated mechanisms in the regulation of energy homeostasis in brain and peripheral tissues

Azúa, Iñigo Ruı́z de; Lutz, Beat

doi:10.1007/s00018-018-2994-6

Cited by 74 publications

(64 citation statements)

References 224 publications

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“…Cannabinoids are known to increase appetite, even in a satiated state, and the consumption of highly palatable food [77]. This orexigenic effect is mediated via CB1 activation in forebrain glutamatergic neurons, hypothalamus, and in a mesolimbic dopamine system [215]. Thus, a pharmacological modulation of CB1 may be used to control food intake [216].…”

Section: Obesitymentioning

confidence: 99%

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A Guide to Targeting the Endocannabinoid System in Drug Design

Stasiulewicz

Znajdek

Grudzień

et al. 2020

IJMS

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The endocannabinoid system (ECS) is one of the most crucial systems in the human organism, exhibiting multi-purpose regulatory character. It is engaged in a vast array of physiological processes, including nociception, mood regulation, cognitive functions, neurogenesis and neuroprotection, appetite, lipid metabolism, as well as cell growth and proliferation. Thus, ECS proteins, including cannabinoid receptors and their endogenous ligands’ synthesizing and degrading enzymes, are promising therapeutic targets. Their modulation has been employed in or extensively studied as a treatment of multiple diseases. However, due to a complex nature of ECS and its crosstalk with other biological systems, the development of novel drugs turned out to be a challenging task. In this review, we summarize potential therapeutic applications for ECS-targeting drugs, especially focusing on promising synthetic compounds and preclinical studies. We put emphasis on modulation of specific proteins of ECS in different pathophysiological areas. In addition, we stress possible difficulties and risks and highlight proposed solutions. By presenting this review, we point out information pivotal in the spotlight of ECS-targeting drug design, as well as provide an overview of the current state of knowledge on ECS-related pharmacodynamics and show possible directions for needed research.

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Section: Obesitymentioning

confidence: 99%

“…This transformation is enhanced either by CB1 inhibition or CB2 activation [214]. Moreover, the CB1 activation promotes adipogenesis, liver lipogenesis, and may exert a pro-inflammatory effect [215] while CB2 mediates inhibition of obese-related inflammation and thus decreases the risk of adverse outcomes in obesity [214].…”

Section: Obesitymentioning

confidence: 99%

A Guide to Targeting the Endocannabinoid System in Drug Design

Stasiulewicz

Znajdek

Grudzień

et al. 2020

IJMS

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“…The levels of circulating endocannabinoids are significantly increased in asthma [47,48], and their ability to modulate the activity of TRPV and TRPM8 channels deserves close attention.…”

Section: Bioactive Lipidsmentioning

confidence: 99%

Dysfunction of transient receptor potential ion channels as an important pathophysiological mechanism in asthma

et al. 2020

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Asthma is a chronic heterogeneous disease characterized by chronic inflammation and bronchial hyperreactivity. Neurogenic inflammation is one of the important causes of hyperreactivity. Dysfunction of transient receptor potential (TRP) ion channels underlies the development of neurogenic inflammation, bronchial hyperreactivity and respiratory symptoms of asthma such as bronchospasm and cough. TRP channels are expressed in the respiratory tract. Their activation is mediated by endogenous and exogenous factors involved in the pathogenesis of asthma. The study of functioning and regulation of TRP channels is relevant, as they could be important therapeutic targets for asthma. The aim of the review is to summarize modern ideas about the mechanisms of functioning and regulation of members of the TRP channel superfamily, the role of which in lung pathology and physiology are the best studied.

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“…6 It appears that the ECS plays roles in the fine-tuning of physiological processes that keep the body in homeostatic set-points. [7][8][9][10] In humans, several polymorphisms in ECS components with associated neuropathophysiological processes have been described, suggesting they promote susceptibility toward development of neuropsychiatric disorders. 11 ECS dysregulation can also be induced by particular life factors, such as living under chronic stress, 12 or by metabolic factors, such as with obesity.…”

Section: Introductionmentioning

confidence: 99%

“…11 ECS dysregulation can also be induced by particular life factors, such as living under chronic stress, 12 or by metabolic factors, such as with obesity. 8 Pharmacological interventions targeting ECS activity aim to normalize such pathophysiological processes, [13][14][15] thereby rescuing the subject from unfavorable allostatic set-points.…”

Section: Introductionmentioning

confidence: 99%

Neurobiology of cannabinoid receptor signaling

Lutz

2020

Dialogues in Clinical Neuroscience

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The endocannabinoid system (ECS) is a highly versatile signaling system within the nervous system. Despite its widespread localization, its functions within the context of distinct neural processes are very well discernable and specific. This is remarkable, and the question remains as to how such specificity is achieved. One key player in the ECS is the cannabinoid type 1 receptor (CB1), a G protein–coupled receptor characterized by the complexity of its cell-specific expression, cellular and subcellular localization, and its adaptable regulation of intracellular signaling cascades. CB1 receptors are involved in different synaptic and cellular plasticity processes and in the brain’s bioenergetics in a context-specific manner. CB2 receptors are also important in several processes in neurons, glial cells, and immune cells of the brain. As polymorphisms in ECS components, as well as external impacts such as stress and metabolic challenges, can both lead to dysregulated ECS activity and subsequently to possible neuropsychiatric disorders, pharmacological intervention targeting the ECS is a promising therapeutic approach. Understanding the neurobiology of cannabinoid receptor signaling in depth will aid optimal design of therapeutic interventions, minimizing unwanted side effects.

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Multiple endocannabinoid-mediated mechanisms in the regulation of energy homeostasis in brain and peripheral tissues

Cited by 74 publications

References 224 publications

A Guide to Targeting the Endocannabinoid System in Drug Design

A Guide to Targeting the Endocannabinoid System in Drug Design

Dysfunction of transient receptor potential ion channels as an important pathophysiological mechanism in asthma

Neurobiology of cannabinoid receptor signaling

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