Tag Archives: CB2

The role of the CB1 receptor in the regulation of sleep.

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“During the 1990s, transmembranal proteins in the central nervous system (CNS) that recognize the principal compound of marijuana, the delta-9-tetrahydrocannabinol (Delta9-THC) were described. The receptors were classified as central or peripheral, CB1 and CB2, respectively. To this date, it has been documented the presence in the CNS of specific lipids that bind naturally to the CB1/CB2 receptors.

The family of endogenous cannabinoids or endocannabinoids comprises oleamide, arachidonoylethanolamine, 2-arachidonylglycerol, virodhamine, noladin ether and N-arachidonyldopamine. Pharmacological experiments have shown that those compounds induce cannabimimetic effects. Endocannabinoids are fatty acid derivates that have a variety of biological actions, most notably via activation of the cannabinoid receptors. The endocannabinoids have an active role modulating diverse neurobiological functions, such as learning and memory, feeding, pain perception and sleep generation.

Experimental evidence shows that the administration of Delta9-THC promotes sleep.

 The activation of the CB1 receptor leads to an induction of sleep, this effect is blocked via the selective antagonist.

Since the system of the endogenous cannabinoids is present in several species, including humans, this leads to the speculation of the neurobiological role of the endocannabinoid system on diverse functions such as sleep modulation.

This review discusses the evidence of the system of the endocannabinoids as well as their physiological role in diverse behaviours, including the modulation of sleep.”

http://www.ncbi.nlm.nih.gov/pubmed/18514375

Beneficial effect of the non-psychotropic plant cannabinoid cannabigerol on experimental inflammatory bowel disease.

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“Inflammatory bowel disease (IBD) is an incurable disease which affects millions of people in industrialised countries. Anecdotal and scientific evidence suggest that Cannabis use may have a positive impact in IBD patients.

 Here, we investigated the effect of cannabigerol (CBG), a non-psychotropic Cannabis-derived cannabinoid, in a murine model of colitis…

  In conclusion, CBG attenuated murine colitis, reduced nitric oxide production in macrophages (effect being modulated by the CB(2) receptor) and reduced ROS formation in intestinal epithelial cells.

CBG could be considered for clinical experimentation in IBD patients.”

http://www.ncbi.nlm.nih.gov/pubmed/23415610

Activation of Cannabinoid CB2 Receptor-Mediated AMPK/CREB Pathway Reduces Cerebral Ischemic Injury.

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“The type 2 cannabinoid receptor (CB2R) was recently shown to mediate neuroprotection in ischemic injury. However, the role of CB2Rs in the central nervous system, especially neuronal and glial CB2Rs in the cortex, remains unclear. We, therefore, investigated anti-ischemic mechanisms of cortical CB2R activation in various ischemic models….

  Collectively, these data demonstrate that cortical CB2R activation by TC (trans-caryophyllene, a CB2R agonist,), ameliorates ischemic injury, potentially through modulation of AMPK/CREB signaling, and suggest that cortical CB2Rs might serve as a putative therapeutic target for cerebral ischemia.”

http://www.ncbi.nlm.nih.gov/pubmed/23414569

Modulation of Cannabinoid Receptor Activation as a Neuroprotective Strategy for EAE and Stroke

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“These results provide evidence that alteration of the activation patterns of the various cannabinoid receptors warrant consideration for future therapeutic strategies.

Interest in the medicinal use of Cannabis sativa (marijuana) has a long historical record, extending back thousands of years. In comparison to the extensive history for medicinal applications of marijuana, the existence of an “endocannabinoid system”, with important homeostatic and pathologic functions, has only recently gained appreciation. The endocannabinoid system consists of endogenously produced cannabinoids, their receptors, and the enzymes responsible for their synthesis and degradation…

Although used in ancient Greece, Rome, and China for therapeutic purposes, concern about the use of cannabinoids as a drug of abuse has dampened interest in developing the potential therapeutic benefits of these compounds. However, a better understanding of the biologic effects has led recently to an upsurge in interest for the development of therapeutic drugs through modification of the endocannabinoid system. An additional incentive was provided by the development of synthetic cannabinoid analogs and specific inhibitors of cannabinoid receptors. Several excellent reviews cover the therapeutic potential of cannabinoids….

The present review is focused on the effects of CB2 receptor activation in models of multiple sclerosis (experimental autoimmune encephalomyelitis) and stroke (middle cerebral occlusion/reperfusion).

In summary, selective CB2 receptor agonists and CB1 receptor antagonists have significant potential for neuroprotection in animal models of two devastating diseases that currently lack effective treatment options.”

Full text: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2855650/

[Expression of cannabinoid receptor 2 in squamous cell carcinoma].

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“The expression of CB2 protein and mRNA levels were detected in normal human skin and squamous cell carcinoma… Both the normal skin and squamous cell carcinoma expressed CB2, which was localized mainly in the basal cell layer and prickle cell layer in human skin with low expressions in the subcutaneous tissue.

 

CONCLUSION:

Squamous cell carcinoma over-expresses CB2 at both the protein and mRNA levels. High expression of CB2 in squamous cell carcinoma suggests an important role of CB2 in the tumorigenesis and development of squamous cell carcinoma.”

http://www.ncbi.nlm.nih.gov/pubmed/20335147

Cannabinoids Induce Apoptosis of Pancreatic Tumor Cells

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 “Pancreatic adenocarcinomas are among the most malignant forms of cancer and, therefore, it is of especial interest to set new strategies aimed at improving the prognostic of this deadly disease. The present study was undertaken to investigate the action of cannabinoids, a new family of potential antitumoral agents, in pancreatic cancer. We show that cannabinoid receptors are expressed in human pancreatic tumor cell lines …

 Cannabinoids… reduced the growth of tumor cells in two animal models of pancreatic cancer. In addition, cannabinoid treatment inhibited the spreading of pancreatic tumor cells. Moreover, cannabinoid administration selectively increased apoptosis and TRB3 expression in pancreatic tumor cells but not in normal tissue… results presented here show that cannabinoids lead to apoptosis of pancreatic tumor cells via a CB2 receptor and de novo synthesized ceramide-dependent up-regulation of p8 and the endoplasmic reticulum stress–related genes ATF-4 and TRB3.

 These findings may contribute to set the basis for a new therapeutic approach for the treatment of pancreatic cancer.

In conclusion, results presented here show that cannabinoids exert a remarkable antitumoral effect on pancreatic cancer cells in vitro and in vivo…

 These findings may help to set the basis for a new therapeutic approach for the treatment of this deadly disease.”

http://www.420magazine.com/forums/pancreatic-cancer/145013-cannabinoids-induce-apoptosis-pancreatic-tumor-cells.html

 

“Cannabinoids Induce Apoptosis of Pancreatic Tumor Cells via Endoplasmic Reticulum Stress–Related Genes“

 

Full text: http://cancerres.aacrjournals.org/content/66/13/6748.long

Chronic blockade of cannabinoid CB2 receptors induces anxiolytic-like actions associated with alterations in GABA(A) receptors.

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“The aim of this study was to explore the effects of CB(2) receptor agonist and antagonist in the regulation of anxiety-like behaviours…The opposing behavioural and molecular changes observed after chronic treatment… support the key role of CB(2) receptors in the regulation of anxiety. Indeed, the efficacy in reducing the anxiety of the spontaneously anxious strain of mice strengthens the potential of the CB(2) receptor as a new target in the treatment of anxiety-related disorders.”

http://www.ncbi.nlm.nih.gov/pubmed/21838753

Overexpression of CB2 cannabinoid receptors decreased vulnerability to anxiety and impaired anxiolytic action of alprazolam in mice.

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“Overexpression of CB2r reduced anxiety-like behaviours in… mice…

 Our findings revealed that increased expression of CB2r significantly reduced anxiogenic-related behaviours, modified the response to stress and impaired the action of anxiolytic drugs.”

http://www.ncbi.nlm.nih.gov/pubmed/20837564

Differential role of anandamide and 2-arachidonoylglycerol in memory and anxiety-like responses.

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“Cannabinoid agonists are potential therapeutic agents because of their antinociceptive and anxiolytic-like effects…

These results dissociate the role of anandamide and 2-arachidonoylglycerol in memory consolidation and anxiety and reveal the interest of cannabinoid receptor 2 as a novel target for the treatment of anxiety-related disorders.”

http://www.ncbi.nlm.nih.gov/pubmed/21684528