Tag Archives: cannabinoid receptors

Cannabinoids – What are Cannabinoids?

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“Cannabinoids are a group of terpenophenolic compounds present in Cannabis (”Cannabis sativa”) and occur naturally in the nervous and immune systems of animals.

The broader definition of cannabinoids refers to a group of substances that are structurally related to tetrahydrocannabinol (THC) or that bind to cannabinoid receptors.

The chemical definition encompasses a variety of distinct chemical classes: the classical cannabinoids structurally related to THC, the nonclassical cannabinoids, the aminoalkylindoles, the eicosanoids related to the endocannabinoids, 1, quinolines and arylsulphonamides, and additional compounds that do not fall into these standard classes but bind to cannabinoid receptors.

The term ”cannabinoids” also refers to a unique group of secondary metabolites found in the cannabis plant, which are responsible for the plant’s peculiar pharmacological effects.

At the present time, there are three general types of cannabinoids: ”phytocannabinoids” occur uniquely in the cannabis plant; ”endogenous cannabinoids” are produced in the bodies of humans and other animals; and ”synthetic cannabinoids” are similar compounds produced in a laboratory.”

http://www.news-medical.net/health/Cannabinoids-What-are-Cannabinoids.aspx

Cannabinoid Receptors

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“Before the 1980s, it was often speculated that cannabinoids produced their physiological and behavioral effects via nonspecific interaction with cell membranes, instead of interacting with specific membrane-bound receptors.

The discovery of the first cannabinoid receptors in the 1980s helped to resolve this debate.

These receptors are common in animals, and have been found in mammals, birds, fish, and reptiles.

At present, there are two known types of cannabinoid receptors, termed CB1 and CB2, with mounting evidence of more.

Cannabinoid receptor type 1

CB1 receptors are found primarily in the brain, to be specific in the basal ganglia and in the limbic system, including the hippocampus.

They are also found in the cerebellum and in both male and female reproductive systems. CB1 receptors are absent in the medulla oblongata, the part of the brain stem responsible for respiratory and cardiovascular functions. Thus, there is not a risk of respiratory or cardiovascular failure as there is with many other drugs. CB1 receptors appear to be responsible for the euphoric and anticonvulsive effects of cannabis.

Cannabinoid receptor type 2

CB2 receptors are almost exclusively found in the immune system, with the greatest density in the spleen.

While found only in the peripheral nervous system, a report does indicate that CB2 is expressed by a subpopulation of microglia in the human cerebellum.

CB2 receptors appear to be responsible for the anti-inflammatory and possibly other therapeutic effects of cannabis.”

http://www.news-medical.net/health/Cannabinoid-Receptors.aspx

Dysregulation of Cannabinoid CB1 Receptor and Associated Signaling Networks in Brains of Cocaine Addicts and Cocaine-Treated Rodents.

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The endocannabinoid system is implicated in the neurobiology of cocaine addiction. This study evaluated the status of cannabinoid CB1 and CB2 receptors, the endocytic cycle of CB1 receptors, receptor regulatory kinases (GRK), and associated signaling (mTOR and p70S6K) in brain cortex of drug abusers and cocaine- and cannabinoid-treated rodents…

 In long-term cocaine addicts, mTOR and p70S6K activations were not altered when compared with controls, indicating that CB1 receptor signaling was dampened. The dysregulation of CB1 receptor, GRK2/3/5, and mTOR/p70S6K signaling by cocaine may contribute to alterations of neuroplasticity and/or neurotoxicity in brains of cocaine addicts.”

More: http://www.ncbi.nlm.nih.gov/pubmed/23727505

Marijuana May Cure PTSD – NBC

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“Veterans suffering from post traumatic stress disorder may find help through marijuana.”

Cannabis Cup Cake Anyone?
  

“Could cannabis cure PTSD?

Post-traumatic stress disorder, which can also affect civilians who undergo a traumatic episode, may be cured by using marijuana, according to an East Bay Express report.

A researcher at Yale University is conducting a long-term study with 120 people — veterans with “intractable cases of PTSD” — who he thinks can be cured of their dehabilitating condition with marijuana.

Most people suffering from PTSD go through a regimen of drugs or more-invasive “exposure therapy,” in which they dig as deeply as possible into their trauma for 12 weeks. Most drop out in Week 3, according to the report.

The theory of R. Andrew Sewell is that tetrahydrocannabinol, or THC, one of the active ingredients in cannabis, can help the brain learn new information. This in turn helps people suffering from PTSD forget the old — as in bad — information.

This is called “extinction learning,” Sewell says. And such learning is made easier when a “switch” in the brain called CB1 is activated. It turns out cannabis is very good at activating the CB1 receptor.

“We’re talking about a cure,” said Sewell, who noted that after treatment, no drugs — not cannabis and not antidepressants — would be required.”

http://www.nbcbayarea.com/news/local/Marijuana-May-Cure-PTSD-208900021.html 

The endocannabinoid system and its therapeutic exploitation.

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“The term ‘endocannabinoid’ – originally coined in the mid-1990s after the discovery of membrane receptors for the psychoactive principle in Cannabis, Delta9-tetrahydrocannabinol and their endogenous ligands – now indicates a whole signalling system that comprises cannabinoid receptors, endogenous ligands and enzymes for ligand biosynthesis and inactivation. This system seems to be involved in an ever-increasing number of pathological conditions. With novel products already being aimed at the pharmaceutical market little more than a decade since the discovery of cannabinoid receptors, the endocannabinoid system seems to hold even more promise for the future development of therapeutic drugs. We explore the conditions under which the potential of targeting the endocannabinoid system might be realized in the years to come.”  http://www.ncbi.nlm.nih.gov/pubmed/15340387

http://www.nature.com/nrd/journal/v3/n9/full/nrd1495.html

Cannabinoids.

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“Since the discovery of an endogenous cannabinoid system, research into the pharmacology and therapeutic potential of cannabinoids has steadily increased. Two subtypes of G-protein coupled cannabinoid receptors, CB(1) and CB(1), have been cloned and several putative endogenous ligands (endocannabinoids) have been detected during the past 15 years. The main endocannabinoids are arachidonoyl ethanolamide (anandamide) and 2-arachidonoyl glycerol (2-AG), derivatives of arachidonic acid, that are produced “on demand” by cleavage of membrane lipid precursors.

 Besides phytocannabinoids of the cannabis plant, modulators of the cannabinoid system comprise synthetic agonists and antagonists at the CB receptors and inhibitors of endocannabinoid degradation. Cannabinoid receptors are distributed in the central nervous system and many peripheral tissues, including immune system, reproductive and gastrointestinal tracts, sympathetic ganglia, endocrine glands, arteries, lung and heart. There is evidence for some non-receptor dependent mechanisms of cannabinoids and for endocannabinoid effects mediated by vanilloid receptors.

Properties of CB receptor agonists that are of therapeutic interest include analgesia, muscle relaxation, immunosuppression, anti-inflammation, antiallergic effects, improvement of mood, stimulation of appetite, antiemesis, lowering of intraocular pressure, bronchodilation, neuroprotection and antineoplastic effects. The current main focus of clinical research is their efficacy in chronic pain and neurological disorders. CB receptor antagonists are under investigation for medical use in obesity and nicotine addiction. Additional potential was proposed for the treatment of alcohol and heroine dependency, schizophrenia, conditions with lowered blood pressure, Parkinson’s disease and memory impairment in Alzheimer’s disease.”

http://www.ncbi.nlm.nih.gov/pubmed/16266285

[The endocannabinoid system].

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“The endocannabinoid system is a physiological system, which is responsible for the control of glucose and lipid-metabolism, as well as for the regulation of the body weight.

 The endocannabinoid receptors are distributed both in the central and peripher nervous system.

Different studies provide evidence that an hyperactive endocannabinoid system is involved in the development of different cardiovascular risk factors.

The pharmacological blockade of these cannabinoid receptors may represent a new approach for cardiometabolic risk management.””

http://www.ncbi.nlm.nih.gov/pubmed/18548817 

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