Tag Archives: CB1

Marijuana-like compound could lead to first-ever medication for PTSD – Fox News

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“The life of an individual suffering from post-traumatic stress disorder (PTSD) is often a debilitating one, as patients are frequently plagued by intense nightmares, flashbacks and emotional instability.   

There are a number of psychotherapeutic treatments and cognitive behavioral therapy options to aid sufferers of PTSD, but these interventions are not always available to patients.  And while medications tend to be the first line of defense for these individuals, no pharmaceutical treatments have been developed yet to specifically target PTSD.

But now, new research may help dramatically change the course of treatment for PTSD patients.  In the first study of its kind, researchers at New York University Langone Medical Center have utilized brain imaging technology to highlight a connection between the number of cannabinoid receptors in the brain and PTSD.  Cannabinoid receptors, known as CB1 receptors, are activated in the brain when a person uses cannabis, which can lead to impaired memory and reduced anxiety.

The researchers’ findings pave the way for the development of the first every medication designed explicitly to treat trauma – something, they say, is desperately needed.”

Read more: http://www.foxnews.com/health/2013/05/14/marijuana-like-compound-could-lead-to-first-ever-medication-for-ptsd/#ixzz2TN3QNhPO

Brain-Imaging Study Links Cannabinoid Receptors to Post-Traumatic Stress Disorder: First Pharmaceutical Treatment for PTSD Within Reach

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“In a first-of-its-kind effort to illuminate the biochemical impact of trauma, researchers at NYU Langone Medical Center have discovered a connection between the quantity of cannabinoid receptors in the human brain, known as CB1 receptors, and post-traumatic stress disorder, the chronic, disabling condition that can plague trauma victims with flashbacks, nightmares and emotional instability…

CB1 receptors are part of the endocannabinoid system, a diffuse network of chemicals and signaling pathways in the body that plays a role in memory formation, appetite, pain tolerance and mood. Animal studies have shown that psychoactive chemicals such as cannabis, along with certain neurotransmitters produced naturally in the body, can impair memory and reduce anxiety when they activate CB1 receptors in the brain…

“There’s not a single pharmacological treatment out there that has been developed specifically for PTSD,” says Dr. Neumeister. “That’s a problem. There’s a consensus among clinicians that existing pharmaceutical treatments such as antidepressant simple do not work. In fact, we know very well that people with PTSD who use marijuana — a potent cannabinoid — often experience more relief from their symptoms than they do from antidepressants and other psychiatric medications. Clearly, there’s a very urgent need to develop novel evidence-based treatments for PTSD.”

Read more: http://www.sciencedaily.com/releases/2013/05/130514085016.htm

Elevated brain cannabinoid CB1 receptor availability in post-traumatic stress disorder: a positron emission tomography study.

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“Endocannabinoids and their attending cannabinoid type 1 (CB1) receptor have been implicated in animal models of post-traumatic stress disorder (PTSD)…

These results suggest that abnormal CB1 receptor-mediated anandamide signaling is implicated in the etiology of PTSD, and provide a promising neurobiological model to develop novel, evidence-based pharmacotherapies for this disorder.”

http://www.ncbi.nlm.nih.gov/pubmed/23670490

Anti-inflammatory cannabinoids in diet: Towards a better understanding of CB(2) receptor action?

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“The endocannabinoid system is an ancient lipid signaling network which in mammals modulates neuronal functions, inflammatory processes, and is involved in the aetiology of certain human lifestyle diseases, such as Crohn’s disease, atherosclerosis and osteoarthritis.

The system is able to downregulate stress-related signals that lead to chronic inflammation and certain types of pain, but it is also involved in causing inflammation-associated symptoms, depending on the physiological context.

The cannabinoid type-2 (CB2) receptor, which unlike the CB1 receptor does not induce central side effects, has been shown to be a promising therapeutic target. While CB1 receptor antagonists/inverse agonists are of therapeutic value, also CB2 receptor ligands including agonists are of pharmacological interest.

 Although the endocannabinoid system is known to be involved in the regulation of energy homoeostasis and metabolism (mainly via CB1 receptors) there was hitherto no direct link between food intake and cannabinoid receptor activation. Our recent finding that beta-caryophyllene, a ubiquitous lipohilic plant natural product, selectively binds to the CB2 receptor and acts as a full agonist is unexpected…

In the case of the dietary natural product beta-caryophyllene, a full CB2 receptor-selective agonist in vitro, potent anti-inflammatory cannabimimetic effects are observed. Intriguingly, the lowest oral dose tested (5 mg/Kg) of this widespread and apparently non-toxic compound, which is also an FDA-approve food additive, was the most effective. Maybe this strengthens the hypothesis that beta-caryophyllene is indeed a dietary cannabinoid, thus inferring that by eating this compound the endocannabinoid system may be modulated in a beneficial way…”

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2633791/

The Cannabinoid 1 Receptor (CNR1) 1359 G/A Polymorphism Modulates Susceptibility to Ulcerative Colitis and the Phenotype in Crohn’s Disease

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“Anecdotal reports suggest that marijuana- or tetrahydrocannabinol-containing products may be effective in alleviating symptoms in patients with ulcerative colitis (UC) and Crohn’s disease (CD). This is supported by recent studies of our group and others suggesting that pharmacological activation of the cannabinoid 1 (CB1) receptor with selective receptor agonists decreases the inflammatory response in various murine models of colonic inflammation…

Recent evidence suggests a crucial role of the endocannabinoid system, including the cannabinoid 1 receptor (CNR1), in intestinal inflammation. We therefore investigated the influence of the CNR1 1359 G/A (p.Thr453Thr; rs1049353) single nucleotide polymorphism (SNP) on disease susceptibility and phenotype in patients with ulcerative colitis (UC) and Crohn’s disease (CD)…

Conclusion

The CNR1 p.Thr453Thr polymorphism appears to modulate UC susceptibility and the CD phenotype. The endocannabinoid system may influence the manifestation of inflammatory bowel diseases, suggesting endocannabinoids as potential target for future therapies.

…our findings provide further evidence that endocannabinoids modulate intestinal inflammation, suggesting that this system could act as a target for future therapeutic interventions.”

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2829088/

Cannabinoid Inhibition of Macrophage Migration to the Trans-Activating (Tat) Protein of HIV-1 Is Linked to the CB2 Cannabinoid Receptor

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“Macrophage-like cells are primary targets for infection by HIV-1…  In the present study, the exogenous cannabinoids δ-9-tetrahydrocannabinol (THC) and (−)-cis-3-[2-hydroxy-4-(1,1-dimethylheptyl)phenyl]-trans-4-(3-hydroxypropyl) cyclohexanol (CP55940) were shown to significantly inhibit migration of human U937 macrophage-like cells to the Tat protein in a concentration-related manner….

Collectively, the pharmacological and biochemical knockdown data indicate that cannabinoid-mediated modulation of macrophage migration to the HIV-1 Tat protein is linked to the CB2 cannabinoid receptor. Furthermore, these results suggest that the CB2 cannabinoid receptor has potential to serve as a therapeutic target for ablation of HIV-1-associated untoward inflammatory response…

,,, the CB2 receptor has the potential to serve as a molecular target for ablating hyperinflammatory responses of macrophage-like cells while avoiding untoward psychotropic effects caused by activation of the CB1 receptor.

 In conclusion, the immunosuppressive and anti-inflammatory properties of select cannabinoids may have profound therapeutic potential in moderating HIV-associated immunopathology, including microglial activation, chemokine/cytokine dysregulation, and monocyte infiltration in the CNS.”

Full text: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2846023/

Cannabinoids may be therapeutic in breast cancer.

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“Cannabinoids are a group of compounds synthesized exclusively by the Cannabis sativa plant, commonly known as marijuana. In 1990, the first cannabinoid-specific membrane (CB1) was characterized and cloned (Matsuda, Lolait, Brownstein, Young, & Bonner, 1990), which catapulted biomedical research on these unique compounds.

 Cannabinoids refer to both marijuana-derived compounds with the active ingredient of 9-tetrahydrocannabinol (THC) and also the synthetic molecules that activate the same primary targets as THC.

Therapeutic properties of marijuana have been well established; however, the clinical use of either plant-sourced or pure cannabinoids remains limited.

The anticachexia properties of cannabinoids are found in tetrahydrocannabinol (oral capsules of synthetically generated THC) and are used to manage weight loss, wasting syndrome, and nausea and vomiting associated with cancer treatment.”

http://www.ncbi.nlm.nih.gov/pubmed/23448745

[The modulatory role of endocannabinoids in sleep].

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“The endogenous cannabinoid, or endocannabinoid, system is present in the central nervous system (CNS) of rodents and humans. This system includes receptors, endogenous ligands and enzymes. The presence of cannabinoid receptors, called CB1, in the CNS has been reported in the cerebral cortex, the hippocampus, the cerebellum and the brain stem. This neuroanatomical location suggests that this receptor could modify several physiological functions, such as the consolidation of memory, motor control and the generation of sleep.

 

Recent reports have described the presence of lipids in the CNS that bind to the CB1 receptor. Administration of said molecules induces cannabimimetic effects, and hence it has been suggested that these lipids are endogenous cannabinoids or endocannabinoids. Anandamide, 2-arachidonylglycerol, virodhamine, noladin ether and N-arachidonyldopamine are molecules that belong to the endocannabinoid family. Anandamide has received more attention from researchers because it was the first endocannabinoid to be reported. Pharmacological experiments have shown that this endocannabinoid induces several different intracellular and behavioural changes.

CONCLUSIONS:

In this study, we review the most important pharmacological aspects of exogenous cannabinoids and the neurobiological role played by the endocannabinoid system, including endogenous and exogenous ligands and receptors. We also examine their pharmacological effects on different behaviours, with particular attention given to the modulation of sleep.”

http://www.ncbi.nlm.nih.gov/pubmed/18297624

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

Expression of the cannabinoid type I receptor and prognosis following surgery in colorectal cancer.

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“The cannabinoid system has been considered to be a potential target of colorectal carcinoma therapy. The aim of this study was to address the correlation between cannabinoid type 1 (CB1) receptor expression and disease severity/outcomes in patients with colorectal cancer (CRC).”

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 “…The high immunoreactivity of the cannabinoid type 1 receptor is a significant prognostic factor following surgery in stage IV CRC…

The effect of cannabinoids in colorectal cancer (CRC) has been demonstrated in in vitro experiments and animal models, which indicate the antiproliferative, apoptotic and antimetastatic actions of cannabinoid agonists…

Antineoplastic effects are mediated by the activation of cannabinoid type I (CB1), type 2 (CB2) or a non-cannabinoid receptor-mediated mechanism…”

Full text: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3576207/