Synthetic and Patented Cannabinoids

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“Historically, laboratory synthesis of cannabinoids were often based on the structure of herbal cannabinoids, and a large number of analogs have been produced and tested, especially in a group led by Roger Adams as early as 1941 and later in a group led by Raphael Mechoulam.

Newer compounds are no longer related to natural cannabinoids or are based on the structure of the endogenous cannabinoids.

Synthetic cannabinoids are particularly useful in experiments to determine the relationship between the structure and activity of cannabinoid compounds, by making systematic, incremental modifications of cannabinoid molecules.

Medications containing natural or synthetic cannabinoids or cannabinoid analogs:

  • Dronabinol (Marinol), is Δ9-tetrahydrocannabinol (THC), used as an appetite stimulant, anti-emetic, and analgesic
  • Nabilone (Cesamet), a synthetic cannabinoid and an analog of Marinol. It is Schedule II unlike Marinol, which is Schedule III
  • Sativex, a cannabinoid extract oral spray containing THC, CBD, and other cannabinoids used for neuropathic pain and spasticity in Canada and Spain. Sativex develops whole-plant cannabinoid medicines
  • Rimonabant (SR141716), a selective cannabinoid (CB1) receptor antagonist used as an anti-obesity drug under the proprietary name Acomplia. It is also used for smoking cessation

Other notable synthetic cannabinoids include:

  • CP-55940, produced in 1974, this synthetic cannabinoid receptor agonist is many times more potent than THC
  • Dimethylheptylpyran
  • HU-210, about 100 times as potent as THC
  • HU-331 a potential anti-cancer drug derived from cannabidiol that specifically inhibits topoisomerase II.
  • SR144528, a CB2 receptor antagonists
  • WIN 55, a potent cannabinoid receptor agonist
  • JWH-133, a potent selective CB2 receptor agonist
  • Levonantradol (Nantrodolum), an anti-emetic and analgesic but not currently in use in medicine”

http://www.news-medical.net/health/Synthetic-and-Patented-Cannabinoids.aspx

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

Cannabis News: The Cannabinoid System Reverses Dementia, Treats PTSD and Controls Diabetes Top May’s News Digest from Publius

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“The Cannabinoid System’s role in reversing dementia, treating PTSD and controlling diabetes highlight May’s cannabis news from Publius, the pen name used by the authors of The Cannabis Papers – Federal ignorance goes on unabated.”

“The Cannabinoid System’s (CS) role in reversing dementia, treating PTSD and controlling diabetes highlight May’s cannabis news from Publius, the pen name used by the authors of The Cannabis Papers: A citizen’s guide to cannabinoids (2011).”

More: http://www.prweb.com/releases/2013/5/prweb10787154.htm

Colombia’s controversial cure for coke addicts: Give them marijuana

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“Marijuana has long been accused of being a gateway to deadlier vices. But could cannabis be a swinging door that might also lead people away from hard drugs? That’s what this capital city is trying to find out.

In a controversial public health project, Bogota will supply marijuana to 300 addicts of bazuco, a cheap cocaine derivative that generates crack-like highs and is as addictive as heroin.

For the most desperate users, the cannabis cure may be the only way out.

“People accuse us of turning bazuco addicts into marijuana addicts but that’s an urban myth,” he said. “This program is about reducing personal harm and the risks to society.”

Authorities believe they might rescue some of the addicts by supplying them with quality controlled medical marijuana with a high THC content (the mind-altering component of marijuana), specifically selected to relieve the anxiety that comes with kicking bazuco.”

More: http://www.thestar.com/news/world/2013/06/03/colombias_controversial_cure_for_coke_addicts_give_them_marijuana.html

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

A Brief History of Medical Marijuana – TIME

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“Should Professors Cheech and Chong ever receive university tenure teaching the medical history of their favorite subject, the course pack would be surprisingly thick.

As early as 2737 B.C., the mystical Emperor Shen Neng of China was prescribing marijuana tea for the treatment of gout, rheumatism, malaria and, oddly enough, poor memory. The drug’s popularity as a medicine spread throughout Asia, the Middle East and down the eastern coast of Africa, and certain Hindu sects in India used marijuana for religious purposes and stress relief. Ancient physicians prescribed marijuana for everything from pain relief to earache to childbirth…

By the late 18th century, early editions of American medical journals recommend hemp seeds and roots for the treatment of inflamed skin, incontinence and venereal disease. Irish doctor William O’Shaughnessy first popularized marijuana’s medical use in England and America. As a physician with the British East India Company, he found marijuana eased the pain of rheumatism and was helpful against discomfort and nausea in cases of rabies, cholera and tetanus.”

http://content.time.com/time/health/article/0,8599,1931247,00.html

Marijuana component can halt brain damage – MSN

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“Extremely low doses of THC – the psychoactive component of marijuana – protects the brain from long-term cognitive damage in case of injury from hypoxia (lack of oxygen), seizures, or toxic drugs, a new study has claimed.

Medical cannabis is often used by sufferers of chronic ailments, including cancer and post-traumatic stress disorder, to combat pain, insomnia, lack of appetite, and other symptoms.

Now, Professor Yosef Sarne of Tel Aviv University”s Adelson Center for the Biology of Addictive Diseases at the Sackler Faculty of Medicine in US found the drug has neuroprotective qualities as well.

Sarne”s current research, published in the journals Behavioural Brain Research and Experimental Brain Research, demonstrates that even extremely low doses of THC – around 1,000 to 10,000 times less than that in a conventional marijuana cigarette – administered over a wide window of 1 to 7 days before or 1 to 3 days after injury can jump start biochemical processes which protect brain cells and preserve cognitive function over time.

This treatment, especially in light of the long time frame for administration and the low dosage, could be applicable to many cases of brain injury and be safer over time, Sarne said.

While performing experiments on the biology of cannabis, researchers found that low doses of the drug had a big impact on cell signalling, preventing cell death and promoting growth factors.

This finding led to a series of experiments designed to test the neuroprotective ability of THC in response to various brain injuries.

In the lab, the researchers injected mice with a single low dose of THC either before or after exposing them to brain trauma. A control group of mice sustained brain injury but did not receive the THC treatment.

When the mice were examined 3 to 7 weeks after initial injury, recipients of the THC treatment performed better in behavioural tests measuring learning and memory.

Additionally, biochemical studies showed heightened amounts of neuroprotective chemicals in the treatment group compared to the control group.

The use of THC can prevent long-term cognitive damage that results from brain injury, the researchers concluded.”

More: http://news.in.msn.com/international/article.aspx?cp-documentid=253106176

Brain Damage can be Prevented by Low Doses Of Marijuana – MedIndia

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“Researchers at Tel Aviv University have found that extremely low doses of THC – the psychoactive component of marijuana – protects the brain from long-term cognitive damage in the wake of injury from hypoxia (lack of oxygen), seizures, or toxic drugs.

Brain damage can have consequences ranging from mild cognitive deficits to severe neurological damage.Previous studies focused on injecting high doses of THC within a very short time frame – approximately 30 minutes – before or after injury.

The current research by Prof. Yosef Sarne of Tel Aviv University’s Adelson Center for the Biology of Addictive Diseases at the Sackler Faculty of Medicine demonstrates that even extremely low doses of THC – around 1,000 to 10,000 times less than that in a conventional marijuana cigarette – administered over a wide window of 1 to 7 days before or 1 to 3 days after injury can jumpstart biochemical processes which protect brain cells and preserve cognitive function over time.

This treatment, especially in light of the long time frame for administration and the low dosage, could be applicable to many cases of brain injury and be safer over time, Prof. Sarne said.

While performing experiments on the biology of cannabis, Prof. Sarne and his fellow researchers discovered that low doses of the drug had a big impact on cell signalling, preventing cell death and promoting growth factors. This finding led to a series of experiments designed to test the neuroprotective ability of THC in response to various brain injuries.

In the lab, the researchers injected mice with a single low dose of THC either before or after exposing them to brain trauma. A control group of mice sustained brain injury but did not receive the THC treatment. When the mice were examined 3 to 7 weeks after initial injury, recipients of the THC treatment performed better in behavioral tests measuring learning and memory. Additionally, biochemical studies showed heightened amounts of neuroprotective chemicals in the treatment group compared to the control group.

The use of THC can prevent long-term cognitive damage that results from brain injury, the researchers concluded.

One explanation for this effect is pre- and post-conditioning, whereby the drug causes minute damage to the brain to build resistance and trigger protective measures in the face of much more severe injury, explained Prof. Sarne.

The low dosage of THC is crucial to initiating this process without causing too much initial damage.

According to Prof. Sarne, there are several practical benefits to this treatment plan. Due to the long therapeutic time window, this treatment can be used not only to treat injury after the fact, but also to prevent injury that might occur in the future.

For example, cardiopulmonary heart-lung machines used in open heart surgery carry the risk of interrupting the blood supply to the brain, and the drug can be delivered beforehand as a preventive measure. In addition, the low dosage makes it safe for regular use in patients at constant risk of brain injury, such as epileptics or people at a high risk of heart attack.

Prof. Sarne is now working in collaboration with Prof. Edith Hochhauser of the Rabin Medical Center to test the ability of low doses of THC to prevent damage to the heart. Preliminary results indicate that they will find the same protective phenomenon in relation to cardiac ischemia, in which the heart muscle receives insufficient blood flow.

His research findings were published in the journals Behavioural Brain Research and Experimental Brain Research.” 

 

Low Doses of THC (Cannabis) Can Halt Brain Damage, Study Suggests – ScienceDaily

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“The use of THC can prevent long-term cognitive damage that results from brain injury, the researchers conclude.

Preventative and long-term use

According to Prof. Sarne, there are several practical benefits to this treatment plan. Due to the long therapeutic time window, this treatment can be used not only to treat injury after the fact, but also to prevent injury that might occur in the future. For example, cardiopulmonary heart-lung machines used in open heart surgery carry the risk of interrupting the blood supply to the brain, and the drug can be delivered beforehand as a preventive measure. In addition, the low dosage makes it safe for regular use in patients at constant risk of brain injury, such as epileptics or people at a high risk of heart attack.

Prof. Sarne is now working in collaboration with Prof. Edith Hochhauser of the Rabin Medical Center to test the ability of low doses of THC to prevent damage to the heart. Preliminary results indicate that they will find the same protective phenomenon in relation to cardiac ischemia, in which the heart muscle receives insufficient blood flow.”

More: http://www.sciencedaily.com/releases/2013/05/130530132531.htm