Tag Archives: cannabinoid receptors

Palmitoylethanolamide: From endogenous cannabimimetic substance to innovative medicine for the treatment of cannabis dependence.

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“Palmitoylethanolamide (PEA) is a fatty acid amide showing some pharmacodynamic similarities with Δ9-tetrahydrocannabinol, the principal psychoactive compound present in the cannabis plant.

Like Δ9-tetrahydrocannabinol, PEA can produce a direct or indirect activation of cannabinoid receptors.

 Furthermore, it acts as an agonist at TRPV1 receptor.

The hypothesis is that PEA has anti-craving effects in cannabis dependent patients, is efficacious in the treatment of withdrawal symptoms, produces a reduction of cannabis consumption and is effective in the prevention of cannabis induced neurotoxicity and neuro-psychiatric disorders.”

http://www.ncbi.nlm.nih.gov/pubmed/23896215

Controlling 2-arachidonoylglycerol metabolism as an anti-inflammatory strategy.

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“The endocannabinoid system is implicated in, and regulates, several physiological processes, ranging from food intake and energy balance to pain and inflammation.

 2-Arachidonoylglycerol (2-AG) is a full agonist at the cannabinoid receptors which classically mediate its effects. The activity of this bioactive lipid is dependent on its endogenous levels, which are tightly controlled by several hydrolases, monoacylglycerol lipase and α/β-hydrolase domain 6 and 12.

 Moreover, 2-AG is also a substrate of cyclooxygenase-2, and this reaction leads to the formation of prostaglandin glycerol esters, the effects of which remain to be fully elucidated.

 In this review we discuss the multiple mechanisms by which 2-AG controls inflammation and the therapeutic potential of 2-AG metabolism inhibitors.”

http://www.ncbi.nlm.nih.gov/pubmed/23891880

The endocannabinoid system in advanced liver cirrhosis: pathophysiological implication and future perspectives.

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“Endogenous cannabinoids (EC) are ubiquitous lipid signalling molecules providing different central and peripheral effects that are mediated mostly by the specific receptors CB1 and CB2. The EC system is highly upregulated during chronic liver disease and consistent experimental and clinical findings indicate that it plays a role in the pathogenesis of liver fibrosis and fatty liver disease associated with obesity, alcohol abuse and hepatitis C.

Furthermore, a considerable number of studies have shown that EC and their receptors contribute to the pathogenesis of the cardio-circulatory disturbances occurring in advanced cirrhosis, such as portal hypertension, hyperdynamic circulatory syndrome and cirrhotic cardiomyopathy.

More recently, the EC system has been implicated in the development of ascites, hepatic encephalopathy and the inflammatory response related to bacterial infection. Rimonabant, a selective CB1 antagonist, was the first drug acting on the EC system approved for the treatment of obesity. Unfortunately, it has been withdrawn from the market because of its neuropsychiatric side effects.

Compounds able to target selectively the peripheral CB1 receptors are under evaluation.

In addition, molecules stimulating CB2 receptor or modulating the activity of enzymes implicated in EC metabolism are promising areas of pharmacological research.

Liver cirrhosis and the related complications represent an important target for the clinical application of these compounds.”

http://www.ncbi.nlm.nih.gov/pubmed/23890208

Anti-inflammatory activity of topical THC in DNFB-mediated mouse allergic contact dermatitis independent of CB1 and CB2 receptors.

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“∆9 -Tetrahydrocannabinol (THC), the active constituent of Cannabis sativa, exerts its biological effects in part through the G-protein-coupled CB1 and CB2 receptors, which were initially discovered in brain and spleen tissue, respectively. However, THC also has CB1/2 receptor-independent effects. Because of its immune-inhibitory potential, THC and related cannabinoids are being considered for the treatment of inflammatory skin diseases.

Here we investigated the mechanism of the anti-inflammatory activity of THC and the role of CB1 and CB2 receptors…

CONCLUSIONS:

Topically applied THC can effectively attenuate contact allergic inflammation by decreasing keratinocyte-derived pro-inflammatory mediators that orchestrate myeloid immune cell infiltration independent of CB1/2 receptors.

This has important implications for the future development of strategies to harness cannabinoids for the treatment of inflammatory skin diseases.”

http://www.ncbi.nlm.nih.gov/pubmed/23889474

Stanford University Study Finds That Marijuana Could Help With Autism

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“A study conducted by Stanford University has found that there might be compounds in marijuana which have some very specific health benefits. The study’s results reveal that cannabinoids – which are found in cannabis – might help to treat autism.”

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“A new study shows that mutations associated with autism block the action of brain molecules that act on the same receptors that marijuana’s active chemical acts on,” according to the Autism Daily Newscast. “Thomas Sudhof, a cellular physiologist at Stanford University, tested mutations associated with autism in mice. Two mutations associated with autism in a synapse-adhesion protein led to deficits in prolonged endocannabinoid signaling in mice. This suggests that autism could caused by a disruption of the brain’s ability to send clear signals.
 
ADN references another study that supports the theory that cannabinoids could be used as a treatment to autism…”
 

More: http://www.opposingviews.com/i/health/stanford-university-study-finds-marijuana-could-help-autism#

Study Finds Cannabis May Provide Treatment For Autism

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“A new study out of Standford University has found promising signs to suggest that cannabinoids – compounds found in cannabis, as well as naturally produced in our body – may help to treat autism.

According to Autism Daily Newscast (ADN); ”A new study shows that mutations associated with autism block the action of brain molecules that act on the same receptors that marijuana’s active chemical acts on”.

They continue: “Thomas Sudhof, a cellular physiologist at Stanford University, tested mutations associated with autism in mice. Two mutations associated with autism in a synapse-adhesion protein led to deficits in prolonged endocannabinoid signaling in mice. This suggests that autism could caused by a disruption of the brain’s ability to send clear signals”.

These findings suggest that cannabinoids could be used as a treatment to autism as they can unblock a disruption in the body’s cannabinoid receptors…”

More: http://www.theweedblog.com/study-finds-cannabis-may-provide-treatment-for-autism/

The Use of Marijuana or Synthetic Cannabinoids for the Treatment of Headache – MedScape

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“Pharmacological preparations of cannabinoid compounds have a variety of therapeutic uses in medicine, including different pain syndromes, but have not been previously reported as beneficial for cluster headache.We present a patient with cluster headache who was refractory to multiple acute and preventive medications but successfully aborted his attacks with recreational marijuana use; subsequent use of dronabinol provided equally effective pain relief. The beneficial effect may be related to the high concentration of cannabinoid receptors in the hypothalamus, which has been implicated as a site of dysfunction in neuroimaging studies of patients with cluster headache.

The plant Cannabis sativa has a long history of medical use in the treatment of pain and spasms, the promotion of sleep, and the suppression of nausea and vomiting. However, in the early 1970s cannabis was classified in the Narcotic Acts in countries all over the world as having no therapeutic benefit; therefore, it cannot be prescribed by physicians or dispensed by pharmacists. In the light of this contradictory situation, an increasing number of patients practice a self-prescription with cannabis products for relieving a variety of symptoms.

  The majority of patients used natural cannabis products such as marihuana, hashish, and an alcoholic tincture; in just 5 cases dronabinol (Marinol) was taken by prescription…

 …this survey demonstrates a successful use of cannabis products for the treatment of a multitude of various illnesses and symptoms. This use was usually accompanied only by slight and in general acceptable side effects…”

http://www.medscape.com/viewarticle/738529

Effects of anandamide in migraine: data from an animal model

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“Endocannabinoid system seems to be involved in the modulation of NTG-induced hyperalgesia, and probably, in the pathophysiological mechanisms of migraine…

The study confirms that a dysfunction of the endocannabinoid system may contribute to the development of migraine attacks and that a pharmacological modulation of CB receptors can be useful for the treatment of migraine pain…

By combining our data with the findings available from the literature, we can hypothesize that a dysfunction of the endocannabinoid system may contribute to the development of migraine attacks and that a specific pharmacological modulation of CB1 and CB2 receptors may be useful for the treatment of migraine pain, without deleterious effects, as well as of specific associated symptoms (nausea, in primis).”

Full text: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3072518/

Role of the cannabinoid system in the transit of beta-amyloid across the blood–brain barrier

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“Emerging evidence suggests beta-amyloid (Aβ) deposition in the Alzheimer’s disease (AD) brain is the result of impaired clearance, due in part to diminished Aβ transport across the blood–brain barrier (BBB). Recently, modulation of the cannabinoid system was shown to reduce Aβ brain levels and improve cognitive behavior in AD animal models…

 The purpose of the current studies was to investigate the role of the cannabinoid system in the clearance of Aβ across the BBB.

  The current studies demonstrate, for the first time, a role for the cannabinoid system in the transit of Aβ across the BBB.

These findings provide insight into the mechanism by which cannabinoid treatment reduces Aβ burden in the AD brain and offer additional evidence on the utility of this pathway as a treatment for AD.”

http://www.sciencedirect.com/science/article/pii/S104474311300064X

Cannabis Use, Effect And Potential Therapy For Alzheimer’s, MS and Parkinson’s

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“The illegal status and wide-spread use of cannabis made basic and clinical cannabis research difficult in the past decades; on the other hand, it has stimulated efforts to identify the psychoactive constituents of cannabis. As a consequence, the endocannabinoid system was discovered, which was shown to be involved in most physiological systems — the nervous, the cardiovascular, the reproductive, the immune system, to mention a few.

One of the main roles of endocannabinoids is neuroprotection, but over the last decade they have been found to affect a long list of processes, from anxiety, depression, cancer development, vasodilatation to bone formation and even pregnancy.

Cannabinoids and endocannabinoids are supposed to represent a medicinal treasure trove which waits to be discovered…

The endocannabinoid system acts as a guardian against various attacks on the mammalian body.

Conclusion

The above described research concerning the endocannabinoid-system is of importance in both basic science and in therapeutics:

  • The discovery of the cannabis plant active constituent has helped advance our understanding of cannabis use and its effects.
  • The discovery of the endocannabinoids has been of central importance in establishing the existence of a new biochemical system and its physiological roles — in particular in neuroprotection.
  • These discoveries have opened the door for the development of novel types of drugs, such as THC for the treatment of nausea and for enhancing appetite in cachectic patients.
  • The endocannabinoid system is involved in the protective reaction of the mammalian body to a long list of neurological diseases such as multiple sclerosis, Alzheimer’s and Parkinson’s disease which raises hope for novel therapeutic opportunities for these diseases.”

More: http://www.sciencedaily.com/releases/2007/10/071014163644.htm