Tag Archives: CB(1) and CB(2) receptors

Cannabinoids as therapeutic agents in cancer: current status and future implications

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“Cannabinoids… active compounds of the Cannabis sativa plant… cannabinoids are clinically used for anti-palliative effects, recent studies open a promising possibility as anti-cancer agents.

They have been shown to possess anti-proliferative and anti-angiogenic effects in vitro as well as in vivo in different cancer models…”  http://www.ncbi.nlm.nih.gov/pubmed/25115386

“Cannabinoids… the active compounds of the Cannabis sativa plant… anti-cancer agents… anti-proliferative… anti-angiogenic… anti-migratory and anti-invasive… The administration of single cannabinoids might produce limited relief compared to the administration of crude extract of plant containing multiple cannabinoids, terpenes and flavanoids.” Full-text: http://www.impactjournals.com/oncotarget/index.php?journal=oncotarget&page=article&op=view&path%5B0%5D=2233&path%5B1%5D=3664

http://www.thctotalhealthcare.com/category/cancer/

[A role for the endocannabinoid system in hepatic steatosis].

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“The endocannabinoid system (SEC) is an important modulator of several metabolic functions.

This system is composed by cannabinoid receptors type 1 and 2 (RCB1 and RCB2), their endogenous ligands, known as endocannabinoids, and the enzymes involved in their synthesis and degradation. A deregulated SEC originates metabolic alterations in several tissues, resulting in the typical manifestations of the metabolic syndrome…

In this review we discuss the proposed mechanisms by which SEC is involved in the etiology of hepatic steatosis, as well as the therapeutic possibilities involving peripheral RCB1/RCB2 antagonism/agonism, for the treatment of this condition.”

http://www.ncbi.nlm.nih.gov/pubmed/25052273

http://www.thctotalhealthcare.com/category/hepatic-steatosis/

The endocannabinoid system: a putative role in neurodegenerative diseases.

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“Scientific evidence shows that an hypofunction or a dysregulation of the endocannabinoid system may be responsible for some of the symptoms of diseases such as multiple sclerosis, amyotrophic lateral sclerosis, Huntington’s, Parkinson’s and Alzheimer’s diseases.

The aim of this review is to highlight the role of endocannabinoid system in neurodegenerative diseases

Scientific evidence shows that cannabis can provide symptomatic relief in several neurodegenerative diseases such as multiple sclerosis, Huntington’s, Parkinson’s and Alzheimer’s diseases, and amyotrophic lateral sclerosis. These findings imply that a hypofunction or a dysregulation of the endocannabinoid system may be responsible for some of the symptoms of these diseases. Moreover, given the abundance of CB1 receptors in areas associated with movement and executive thought, researchers’ interest has often focused on endocannabinoid levels in patients with motor degenerative disorders.

CONCLUSIONS:

The important role played by endocannabinoid system promises interesting developments, in particular to evaluate the effectiveness of new drugs in both psychiatry and neurology.”

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4070159/

CANNABINOIDs INHIBIT angiogenic capacities of Endothelial cells via release of Tissue inhibitor of matrix metalloproteinases-1 from lung cancer cells.

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“Cannabinoids inhibit tumor neovascularisation as part of their tumorregressive action.

However, the underlying mechanism is still under debate. In the present study the impact of cannabinoids on potential tumor-to-endothelial cell communication conferring anti-angiogenesis was studied…

Collectively, our data suggest a pivotal role of the anti-angiogenic factor TIMP-1 inintercellular tumor-endothelial cell communication resulting in anti-angiogenic features of endothelial cells.”

http://www.ncbi.nlm.nih.gov/pubmed/24976505

http://www.thctotalhealthcare.com/category/lung-cancer/

The Cannabinoid WIN55212-2 Promotes Neural Repair After Neonatal Hypoxia–Ischemia

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Figure 1.

“In the last years, cannabinoids have emerged as promising neuroprotective agents in several animal paradigms of acute and degenerative brain damage. Most neuroprotective effects of cannabinoids result from the activation of cannabinoid Type 1 (CB1R) and Type 2 (CB2R) receptors in neural and immune cells.

Besides, the stimulating effect of cannabinoids on proliferation, survival, and differentiation of neural progenitor cells provides interesting prospects for long-term neural repair after acute brain damage.

The endocannabinoid system has been involved in the modulation of neural stem cells proliferation, survival and differentiation as well as in the generation of new oligodendrocyte progenitors in the postnatal brain. The present work aims to test the effect of the synthetic Type 1 and Type 2 cannabinoid receptor agonist WIN55212-2 on these processes in the context of neonatal rat brain hypoxia–ischemia (HI)…

Our results suggest that the activation of the endocannabinoid system promotes white and gray matter recovery after neonatal HI injury…

In conclusion, we have demonstrated that the synthetic cannabinoid WIN55212-2 enhances SVZ cell proliferation, oligodendrogenesis, white matter remyelination, and neuroblast generation after neonatal HI.

These findings, summed to the previously described neuroprotective properties of cannabinoids after acute brain damage, may possess therapeutic repercussions in the long-term management of neonatal HI encephalopathy, a prevalent and devastating condition for which no pharmacological treatments are yet available.”

http://stroke.ahajournals.org/content/41/12/2956.full

 

Activation of cannabinoid 2 receptors protects against cerebral ischemia by inhibiting neutrophil recruitment

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“THE CONSEQUENCES OF ISCHEMIC INJURY in liver, heart, and brain can be ameliorated by cannabinoids, a group of diverse compounds that include constituents of the plant Cannabis sativa (phytocannabinoids), endogenous lipids (endocannabinoids), and synthetic substances. Most of the effects of cannabinoids are mediated by the G-protein-coupled receptors cannabinoid receptor 1 (CB1) and cannabinoid receptor 2 (CB2)… 

Cannabinoids protect against ischemic stroke…

Activation of the cannabinoid 2 receptor (CB2) reduces ischemic injury in several organs…

In conclusion, our data demonstrate that by activating p38 in neutrophils, CB2 agonists inhibit neutrophil recruitment to the brain and protect against ischemic brain injury.”

http://www.fasebj.org/content/24/3/788.long

Researchers Meet to Discuss Cannabinoid-Based Stroke Therapy

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Murikinati et al., 2010 shows that brain tissue is saved after a stroke with JWH-133

“The Cannabinoid Discussion Group at Temple University met for the second time this semester to review a recent scientific publication from a German Laboratory. The presenter was Zachary Reichenbach, an MD/Ph.D student at Temple, who is currently working in the laboratory of Dr.Ron Tuma. The Tuma lab is focused on studying cannabinoid based therapies for the treatment of cerebral ischemia resulting from stroke. Mr.Reichenbach led the discussion on a research paper which showed that the cannabinoid JWH-133 activates the cannabinoid type 2 receptor (CB2R), resulting a decrease in infarct size or brain damage duringreperfusion following an ischemic event.

Mr.Reichenbach provided background on stroke, stating that it is the 3rd cause of death in this country, and 85% of those strokes are of the ischemic variety. During an ischemic event there is a hyper-immune response resulting in the recruitment of immune cells that kill brain tissue. Cannabinoids have been shown to modulate the immune system, notably the Tuma lab has published data on the CB2 receptor’s anti-inflammatory effects. Activating the CB2 receptor decreases the migration of hyper-immune cells to the brain. The more brain you save, the more you save someone from disabilities or death.

When asked about the implications of these findings on a cannabinoid that could be a potential stroke therapy, Mr.Reichenbach replied that the results of his work and others is promising…

And just in case you were wondering, THC, the active ingredient in Cannabis, activates both the CB1 and CB2 receptor.”

http://www.examiner.com/article/researchers-meet-to-discuss-cannabinoid-based-stroke-therapy

Cannabinoids and Neuroprotection in Stroke

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“One of the most recently described neural signaling systems is that mediated by endogenous cannabinoids (endocannabinoids). Cannabinoids have recently been shown to attenuate neuronal injury induced by hypoxia and glucose deprivation in cell culture, as well as injury induced in rat brain following both global and focal cerebral ischemia in vivo.

Two endocannabinoids have been characterized in detail: N-arachidonylethanolamide and 2-arachidonylglycerol. Cannabinoid CB1 and CB2receptors have been cloned and an alternatively spliced CB1A isoform has been identified.

The development of metabolically stable, synthetic, enantiomeric cannabinoid receptor agonists and of CB1 and CB2 receptor antagonists has greatly aided the characterization of cannabinoid receptor-mediated processes, although certain aspects of cannabinoid signaling in some systems remain poorly understood.

Indirect evidence suggests that cannabinoids might serve as endogenous regulators of ischemic neuronal injury, but several recent reports provide more direct evidence bearing on such a role.

The author’s own findings provide evidence for CB1 receptor-mediated neuroprotection in vivo, but non-receptor-mediated protection in vitro.”

http://journals.prous.com/journals/servlet/xmlxsl/pk_journals.xml_summary_pr?p_JournalId=3&p_RefId=129&p_IsPs=Y

Cannabis Counter Brain Cell Damage After a Stroke

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“New research by University of Otago scientists suggests some mechanisms in the brain targeted by cannabis could become drugs targets to counter brain cell damage after a stroke.

Researchers from the Medical School’s Department of Pharmacology and Toxicology have been the first in the world to show the cannabinoid CB2 receptor appears in the rat brain following a stroke.

Their findings were published recently in the journal Neuroscience Letters.

Dr John Ashton says the CB2 receptor is a protein produced as part of the body’s immune response system.

“This response is triggered by stroke and causes the inflammation that leads to damage in the area of the brain around where the stroke has occurred.

“If the inflammation can be stopped or reduced then it offers the hope of reducing the extent of the damage caused by stroke – and CB2 offers a potential target for such a drug.”

Dr Ashton says cannabis targets both the CB2 and the related CB1 receptors.

“THC, the major active ingredient of cannabis, acts mainly on CB1 but it also affects CB2. While THC is known to have some positive effects in terms of pain management its use is severely limited because of the way it triggers the psychoactive CB1 receptors in the brain,” he says.

“The aim would be to develop a drug that targets the CB2 receptor without affecting CB1.”

Dr Ashton says the relationship between cannabis and cannabinoid drugs has similarities to the relationship between heroin and codeine.

“Heroin and codeine share common targets, but by designing codeine in such a way that it eliminated the psychoactive side-effects seen with heroin, a therapeutically useful drug was developed. There is the potential to do the same with cannabinoids.”

Drugs targeting CB2 could also have potential therapeutic use in other conditions involving inflammatory damage to the brain, such as Huntington’s Disease and Alzheimer’s Disease. There may also be scope to use them in pain management.

“CB2 cells are also found in the spinal cord. They regulate pain signals making them a potential target for new pain killing drugs.””

http://www.hightimes.com/read/cannabis-counter-brain-cell-damage-after-stroke

Cannabinoids drug for inflammatory bowel

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Medindia

“Researchers from the University of Bath, UK has found that Cannabinoids derived from Cannabis has found to be effective in the treatment of inflammatory bowel diseases like Crohn’s disease and ulcerative colitis.

“The system that responds to cannabis in the brain is present and functioning in the lining of the gut,” lead researcher Dr. Karen Wright, of the University of Bath, explained to Reuters Health. “There is an increased presence of one component of this system during inflammatory bowel diseases,” she explained.

The report of the study was published in the Journal of Gastroenterology in which she has explained the location of CB1 and CB2 receptors in human colon tissue which binds to the Cannabinoid. She has used Human colon cell lines to establish the binding of the cannabinoid compounds and in her wound healing experiments.

Increased CB2 receptors are found in colonic tissue characteristic of inflammatory bowel disease. They found that the Cannabinoids helps in wound healing of the surface by CB1 related receptor mechanism.

“Cannabinoids, which we make ourselves, as well as synthetic Cannabinoids, can promote wound healing in the gut, which is extremely interesting given that inflammatory bowel disease involves damaged gut linings,” Wright said.”

http://www.medindia.net/news/view_news_main.asp?x=4578