Tag Archives: cannabinoid receptors

Anti-Obesity Effect of the CB2 Receptor Agonist JWH-015 in Diet-Induced Obese Mice.

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“The cannabinoid receptor 2 (CB2) is well known for its immune modulatory role. However, recent localisation of CB2 receptors in metabolically active tissue suggests that the CB2 receptor plays a significant role in energy homeostasis.

This study was designed to investigate the impact of chronic CB2 receptor stimulation on food intake, body weight and mood.

These results demonstrate a role for CB2 receptors in modulating energy homeostasis and obesity associated metabolic pathologies in the absence of any adverse impact on mood.”

http://www.ncbi.nlm.nih.gov/pubmed/26588700

Controlled release tablet formulation containing natural δ9 tetrahydrocannabinol.

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“Cannabinoids are increasingly being used in the treatment of chemotherapy induced nausea and vomiting (CINV) because of their action on the cannabinoid receptors, CB1 and CB2.

The currently marketed capsule formulations (sesame oil based and crystalline powder) are required to be administered frequently to maintain therapeutic levels, which leads to non-compliance.

In the present study, oral controlled release tablet formulations of Δ9- tetrahydrocannabinol (THC) were prepared using the lipids Precirol® and Compritrol®. Release profiles using THC-lipid matrices and/or with the lipids in the external phase (blend) were evaluated…

The overall results demonstrate the feasibility of preparing oral THC tablets for once a day administration which can improve CINV management.”

http://www.ncbi.nlm.nih.gov/pubmed/26585693

Pharmacological benefits of selective modulation of cannabinoid receptor type 2 (CB2) in experimental Alzheimer’s disease.

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“Alzheimer’s disease (AD) is a progressive neurodegenerative disorder that pervasively affects the population across the world.

Currently, there is no effective treatment available for this and existing drugs merely slow the progression of cognitive function decline. Thus, massive effort is required to find an intended therapeutic target to overcome this condition.

The present study has been framed to investigate the ameliorative role of selective modulator of cannabinoid receptor type 2 (CB2), 1-phenylisatin in experimental AD condition…

Hence, this study concludes that CB2 receptor modulation can be a potential therapeutic target for the management of AD.”

http://www.ncbi.nlm.nih.gov/pubmed/26577751

The effect of five day dosing with THCV on THC-induced cognitive, psychological and physiological effects in healthy male human volunteers: A placebo-controlled, double-blind, crossover pilot trial.

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“Cannabis is mostly grown under illegal and unregulated circumstances, which seems to favour a product increasingly high in its main cannabinoid ∆-9-tetrahydrocannabinol (THC). ∆-9-tetrahydrocannabivarin (THCV) is a relatively untested cannabinoid which is said to be a cannabinoid receptor neutral antagonist, and may inhibit the effects of THC.

In this first study of THC and THCV, THCV inhibited some of the well-known effects of THC, while potentiating others.”

http://www.ncbi.nlm.nih.gov/pubmed/26577065

 

The cannabinoid system in the retrosplenial cortex modulates fear memory consolidation, reconsolidation, and extinction.

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“Despite the fact that the cannabinoid receptor type 1 (CB1R) plays a pivotal role in emotional memory processing in different regions of the brain, its function in the retrosplenial cortex (RSC) remains unknown. Here, using contextual fear conditioning in rats, we showed that a post-training intra-RSC infusion of the CB1R antagonist AM251 impaired, and the agonist CP55940 improved, long-term memory consolidation. Additionally, a post-reactivation infusion of AM251 enhanced memory reconsolidation, while CP55940 had the opposite effect. Finally, AM251 blocked extinction, whereas CP55940 facilitated it and maintained memory extinguished over time. Altogether, our data strongly suggest that the cannabinoid system of the RSC modulates emotional memory.”

http://www.ncbi.nlm.nih.gov/pubmed/26572648

Seeing over the horizon – targeting the endocannabinoid system for the treatment of ocular disease.

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“The observation that marijuana reduces intraocular pressure was made by Hepler and Frank in the 1970s. Since then, there has been a significant body of work investigating cannabinoids for their potential use as therapeutics.

To date, no endocannabinoid system (ECS)-modulating drug has been approved for clinical use in the eye; however, recent advances in our understanding of the ECS, as well as new pharmacological tools, has renewed interest in the development of ocular ECS-based therapeutics.

This review summarizes the current state-of-affairs for the use of ECS-modulating drugs for the treatment of glaucoma and ocular inflammatory and ischemic disease.”

http://www.ncbi.nlm.nih.gov/pubmed/26565550

Cannabinoid CB1 receptors and mTORC1 signalling pathway interact to modulate glucose homeostasis.

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“The endocannabinoid system (ECS) is an inter-cellular signalling mechanism that is present in the islets of Langerhans and plays a role in the modulation of insulin secretion and beta-cell mass expansion.

The mammalian target of rapamycin complex 1 (mTORC1) is a key intra-cellular pathway involved in energy homeostasis and known to importantly affect pancreatic islet’s physiology.

These findings suggest a functional interaction between the ECS and the mTORC1 pathway within the endocrine pancreas and at the whole organism level, which could have implications for the development of new therapeutic approaches for pancreatic beta-cell diseases.”

http://www.ncbi.nlm.nih.gov/pubmed/26563389

Endocannabinoid regulation of nausea is mediated by 2-arachidonoylglycerol (2-AG) in the rat visceral insular cortex.

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“Cannabinoid (CB) agonists suppress nausea in humans and animal models; yet, their underlying neural substrates remain largely unknown.

Evidence suggests that the visceral insular cortex (VIC) plays a critical role in nausea. Given the expression of CB1 receptors and the presence of endocannabinoids in this brain region, we hypothesized that the VIC endocannabinoid system regulates nausea…

Taken together, these findings provide compelling evidence that acute nausea selectively increases 2-AG in the VIC, and suggests that 2-AG signaling within the VIC regulates nausea by reducing neuronal activity in this forebrain region.”

Clinical Significance of Cannabinoid Receptors CB1 and CB2 Expression in Human Malignant and Benign Thyroid Lesions.

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“The endocannabinoid system is comprised of cannabinoid receptors (CB1 and CB2), their endogenous ligands (endocannabinoids), and proteins responsible for their metabolism participate in many different functions indispensable to homeostatic regulation in several tissues, exerting also antitumorigenic effects.

The present study aimed to evaluate the clinical significance of CB1 and CB2 expression in human benign and malignant thyroid lesions.

Our data suggest that CB receptors may be involved in malignant thyroid transformation and especially CB2 receptor could serve as useful biomarker and potential therapeutic target in thyroid neoplasia.”

http://www.ncbi.nlm.nih.gov/pubmed/26539529

http://www.hindawi.com/journals/bmri/2015/839403/

Activation of Endocannabinoid System Is Associated with Persistent Inflammation in Human Aortic Aneurysm.

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“Human aortic aneurysms have been associated with inflammation and vascular remodeling. Since the endocannabinoid system modulates inflammation and tissue remodeling, we investigated its components in human aortic aneurysms…

Our data provides evidence for endocannabinoid system activation in human aortic aneurysms, associated with persistent low-level inflammation and vascular remodeling.”

http://www.ncbi.nlm.nih.gov/pubmed/26539497