Tag Archives: cannabidiol

GW Pharmaceuticals: Giving New Meaning To ‘High Potential’

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“GW Pharmaceuticals (GWPH) is an UK-based biopharmaceutical company focused on the discovery and development of cannabinoid-based products for a wide range of indications. GW has established a technology platform based on genetically modified cannabis plants and has become a leader in plant-derived cannabinoid therapeutics.

 GW’s lead program is Sativex, a cannabis extract based oromucosal spray whose main actives are the cannabinoids delta-9- tetrahydrocannabinol (THC), and cannabidiol (CBD). It is approved for the treatment of multiple sclerosis (MS) spasticity in 21 countries outside of the U.S and already marketed in seven countries (eight following Italian launch in Q213).

…While MS spasticity has provided proof-of-concept in the worldwide approvability of Sativex, a more meaningful commercial opportunity is in the treatment of opioid-refractory cancer pain. Sativex has been tested in two Phase II trials in cancer pain. The trials have demonstrated that Sativex is safe and effective when used in addition to opioids in patients whose cancer pain is not sufficiently managed by opioids alone. Based on these results, GW has initiated three Phase III trials. The first two are expected to complete during 2014 and support an FDA filing.”

More: http://seekingalpha.com/article/1490392-gw-pharmaceuticals-giving-new-meaning-to-high-potential

Marijuana Derivative May Offer Hope in Cocaine Addiction – TIME

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“A new study in mice has found that activating a receptor affected by marijuana can dramatically reduce cocaine consumption. The research suggests that new anti-addiction drugs might be developed using synthetic versions of cannabidiol (CBD), the marijuana component that activates the receptor—or even by using the purified natural compound itself.

Researchers formerly believed that the receptor, known as CB2, was not found in the brain and that therefore CBD had no psychoactive effects. But a growing body of research suggests otherwise. After THC, CBD is the second most prevalent active compound in marijuana.”

More: http://healthland.time.com/2011/07/26/marijuana-derivative-may-offer-hope-in-cocaine-addiction/

Could Marijuana Treat Schizophrenia?

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“Researchers find cannabidiol is as effective as standard antipsychotic drugs—with fewer side effects.”

A compound found in marijuana can help treat schizophrenia as effectively as standard antipsychotic drugs—and with fewer side effects—according to the results of a new clinical trial, reports The Fix columnist Maia Szalavitz in Time. Researchers at University of Cologne in Germany studied 39 people with schizophrenia, all hospitalized for a psychotic episode. Twenty of the patients were given cannabidiol (CBD), a substance found in marijuana that is associated with its mellowing, anti-anxiety effects (not THC—the main ingredient in marijuana, which has been found to worsen schizophrenia). The other participants were given amisulpride, an antipsychotic medication. At the end of the four-week trial, both groups showed significant clinical improvement in their schizophrenic symptoms. “The results were amazing,” says Daniele Piomelli, professor of pharmacology at the University of California-Irvine and a co-author of the study. “Not only was [CBD] as effective as standard antipsychotics, but it was also essentially free of the typical side effects seen with antipsychotic drugs.” Antipsychotic medications can cause serious, sometimes permanent movement disorders and other side effects such as weight gain and movement problems. In the study, these side effects were observed in those taking amisulpride, but not in those taking CBD. “These exciting findings should stimulate a great deal of research,” says Dr. John Krystal, chair of psychiatry at Yale University School of Medicine, who was not associated with the study. He noted that CBD, in addition to having fewer side effects, also seemed to work better on schizophrenia’s negative symptoms, which are notoriously difficult to treat, including: social withdrawal, blunting of pleasure, and lack of motivation.”

http://www.thefix.com/content/pot-compound-treats-schizophrenia-few-side-effects91717

Cannabidiol (CBD): Fighting Inflammation & Aggressive Forms of Cancer

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“Marijuana contains at least 60 known chemicals called cannabinoids, which activate cannabinoid receptors in your body. Tetrahydrocannabinol, or THC, is the main component responsible for the psychoactive effects, or “high,” marijuana is known for. While THC is known to have some medicinal value, there has been recent investigation into a new cannabinoid that is rumored to have more medicinal benefits than any single pharmaceutical drug on the market.”

“What is Cannabidiol (CBD)?

This cannabinoid is known as Cannabidiol (CBD), and is the second most abundant cannabinoid in cannabis. Research done by G.W. Pharmaceuticals suggests that CBD could be used for treating symptoms of rheumatoid arthritis and other autoimmune diseases, diabetes, nausea, bowel disorders, and many other hard-to-control side effects. According to an article from Projectcbd.com, CBD has even demonstrated neuroprotective effects, and its anti-cancer potential is currently being explored.

While it was originally believed that THC is a breakdown product of CBD, it is now known that both THC and CBD are actually metabolites of their decarboxylated acidic forms, THCa and CBDa. These acidic precursors are decarboxylated (essentially dried) by heat or extraction to produce THC and CBD; only then do they become psychoactive. The compound has medicinal benefits without the “high” that some patients do not desire. This makes CBD appealing to patients who are looking for an alternative to their current meds, which often have opiate-like effects.”

More: http://www.medicaljane.com/2012/12/20/cannabidiol-cbd-medicine-of-the-future/

Phytocannabinoids

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“Phytocannabinoids, also called ”natural cannabinoids”, ”herbal cannabinoids”, and ”classical cannabinoids”, are only known to occur naturally in significant quantity in the cannabis plant, and are concentrated in a viscous resin that is produced in glandular structures known as trichomes.

In addition to cannabinoids, the resin is rich in terpenes, which are largely responsible for the odour of the cannabis plant.

Phytocannabinoids are nearly insoluble in water but are soluble in lipids, alcohols, and other non-polar organic solvents. However, as phenols, they form more water-soluble phenolate salts under strongly alkaline conditions.

All-natural cannabinoids are derived from their respective 2-carboxylic acids (2-COOH) by decarboxylation (catalyzed by heat, light, or alkaline conditions).

Types

At least 66 cannabinoids have been isolated from the cannabis plant. To the right the main classes of natural cannabinoids are shown. All classes derive from cannabigerol-type compounds and differ mainly in the way this precursor is cyclized.

Tetrahydrocannabinol (THC), cannabidiol (CBD) and cannabinol (CBN) are the most prevalent natural cannabinoids and have received the most study. Other common cannabinoids are listed below:

  • CBG Cannabigerol
  • CBC Cannabichromene
  • CBL Cannabicyclol
  • CBV Cannabivarin
  • THCV Tetrahydrocannabivarin
  • CBDV Cannabidivarin
  • CBCV Cannabichromevarin
  • CBGV Cannabigerovarin
  • CBGM Cannabigerol Monoethyl Ether

Tetrahydrocannabinol

Tetrahydrocannabinol (THC) is the primary psychoactive component of the plant. It appears to ease moderate pain (analgetic) and to be neuroprotective. THC has approximately equal affinity for the CB1 and CB2 receptors. Its effects are perceived to be more cerebral.

”Delta”-9-Tetrahydrocannabinol (Δ9-THC, THC) and ”delta”-8-tetrahydrocannabinol (Δ8-THC), mimic the action of anandamide, a neurotransmitter produced naturally in the body. The THCs produce the ”high” associated with cannabis by binding to the CB1 cannabinoid receptors in the brain.

Cannabidiol

Cannabidiol (CBD) is not psychoactive, and was thought not to affect the psychoactivity of THC. However, recent evidence shows that smokers of cannabis with a higher CBD/THC ratio were less likely to experience schizophrenia-like symptoms.

This is supported by psychological tests, in which participants experience less intense psychotic effects when intravenous THC was co-administered with CBD (as measured with a PANSS test).

It has been hypothesized that CBD acts as an allosteric antagonist at the CB1 receptor and thus alters the psychoactive effects of THC.

It appears to relieve convulsion, inflammation, anxiety, and nausea. CBD has a greater affinity for the CB2 receptor than for the CB1 receptor.

Cannabigerol

Cannabigerol (CBG) is non-psychotomimetic but still affects the overall effects of Cannabis. It acts as an α2-adrenergic receptor agonist, 5-HT1A receptor antagonist, and CB1 receptor antagonist. It also binds to the CB2 receptor.

Tetrahydrocannabivarin

Tetrahydrocannabivarin (THCV) is prevalent in certain South African and Southeast Asian strains of Cannabis. It is an antagonist of THC at CB1 receptors and attenuates the psychoactive effects of THC.

Cannabichromene

Cannabichromene (CBC) is non-psychoactive and does not affect the psychoactivity of THC It is found in nearly all tissues in a wide range of animals.

Two analogs of anandamide, 7,10,13,16-docosatetraenoylethanolamide and ”homo”-γ-linolenoylethanolamine, have similar pharmacology.

All of these are members of a family of signalling lipids called ”N”-acylethanolamides, which also includes the noncannabimimetic palmitoylethanolamide and oleoylethanolamine, which possess anti-inflammatory and orexigenic effects, respectively. Many ”N”-acylethanolamines have also been identified in plant seeds and in molluscs.

  • 2-arachidonoyl glycerol (2-AG)

Another endocannabinoid, 2-arachidonoyl glycerol, binds to both the CB1 and CB2 receptors with similar affinity, acting as a full agonist at both, and there is some controversy over whether 2-AG rather than anandamide is chiefly responsible for endocannabinoid signalling ”in vivo”.

In particular, one ”in vitro” study suggests that 2-AG is capable of stimulating higher G-protein activation than anandamide, although the physiological implications of this finding are not yet known.

  • 2-arachidonyl glyceryl ether (noladin ether)

In 2001, a third, ether-type endocannabinoid, 2-arachidonyl glyceryl ether (noladin ether), was isolated from porcine brain.

Prior to this discovery, it had been synthesized as a stable analog of 2-AG; indeed, some controversy remains over its classification as an endocannabinoid, as another group failed to detect the substance at “any appreciable amount” in the brains of several different mammalian species.

It binds to the CB1 cannabinoid receptor (”K”i = 21.2 nmol/L) and causes sedation, hypothermia, intestinal immobility, and mild antinociception in mice. It binds primarily to the CB1 receptor, and only weakly to the CB2 receptor.

Like anandamide, NADA is also an agonist for the vanilloid receptor subtype 1 (TRPV1), a member of the vanilloid receptor family.

  • Virodhamine (OAE)

A fifth endocannabinoid, virodhamine, or ”O”-arachidonoyl-ethanolamine (OAE), was discovered in June 2002. Although it is a full agonist at CB2 and a partial agonist at CB1, it behaves as a CB1 antagonist ”in vivo”.

In rats, virodhamine was found to be present at comparable or slightly lower concentrations than anandamide in the brain, but 2- to 9-fold higher concentrations peripherally.

Function

Endocannabinoids serve as intercellular ‘lipid messengers’, signaling molecules that are released from one cell and activate the cannabinoid receptors present on other nearby cells.

Although in this intercellular signaling role they are similar to the well-known monoamine neurotransmitters, such as acetylcholine and dopamine, endocannabinoids differ in numerous ways from them. For instance, they use retrograde signaling.

Furthermore, endocannabinoids are lipophilic molecules that are not very soluble in water. They are not stored in vesicles, and exist as integral constituents of the membrane bilayers that make up cells. They are believed to be synthesized ‘on-demand’ rather than made and stored for later use.

The mechanisms and enzymes underlying the biosynthesis of endocannabinoids remain elusive and continue to be an area of active research.

The endocannabinoid 2-AG has been found in bovine and human maternal milk.

Retrograde signal

Conventional neurotransmitters are released from a ‘presynaptic’ cell and activate appropriate receptors on a ‘postsynaptic’ cell, where presynaptic and postsynaptic designate the sending and receiving sides of a synapse, respectively.

Endocannabinoids, on the other hand, are described as retrograde transmitters because they most commonly travel ‘backwards’ against the usual synaptic transmitter flow.

They are, in effect, released from the postsynaptic cell and act on the presynaptic cell, where the target receptors are densely concentrated on axonal terminals in the zones from which conventional neurotransmitters are released.

Activation of cannabinoid receptors temporarily reduces the amount of conventional neurotransmitter released.

This endocannabinoid mediated system permits the postsynaptic cell to control its own incoming synaptic traffic.

The ultimate effect on the endocannabinoid-releasing cell depends on the nature of the conventional transmitter being controlled.

For instance, when the release of the inhibitory transmitter GABA is reduced, the net effect is an increase in the excitability of the endocannabinoid-releasing cell.

On the converse, when release of the excitatory neurotransmitter glutamate is reduced, the net effect is a decrease in the excitability of the endocannabinoid-releasing cell.

Range

Endocannabinoids are hydrophobic molecules. They cannot travel unaided for long distances in the aqueous medium surrounding the cells from which they are released, and therefore act locally on nearby target cells. Hence, although emanating diffusely from their source cells, they have much more restricted spheres of influence than do hormones, which can affect cells throughout the body.

Other thoughts

Endocannabinoids constitute a versatile system for affecting neuronal network properties in the nervous system.

”Scientific American” published an article in December 2004, entitled “The Brain’s Own Marijuana” discussing the endogenous cannabinoid system.

The current understanding recognizes the role that endocannabinoids play in almost every major life function in the human body.

U.S. Patent # 6630507

In 2003 The U.S.A.’s Government as represented by the Department of Health and Human Services was awarded a patent on cannabinoids as antioxidants and neuroprotectants. U.S. Patent 6630507.”

http://www.news-medical.net/health/Phytocannabinoids.aspx

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

Fighting Cancer: Another Study Reveals the Cannabis and Cancer Prevention Link

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“Does marijuana cause cancer? Revealing the link between cannabis and cancer yet again, researchers with the California Pacific Medical Center in San Francisco have released findings that further bolster cannabis as an anti-cancer solution.
The researchers have found a compound in the much-talked-about plant could “halt the spread” of many types of aggressive cancers, including breast cancer.

The Cannabis and Cancer Link

Cannabidiol is the compound, and while it fights cancer cells, it does not produce the high feelings commonly associated with cannabis. Instead, it seems to “switch off” the gene responsible for metastasizing breast cancer.

They reportedly found the compound doesn’t only stop the breast cancer cells from growing, but even causes them to return back to normal cells, cancer-free.”

More: http://naturalsociety.com/study-positive-cannabis-and-cancer-link/

Medical Marijuana Inc Announces Positive Developments in Recent Studies Using Cannabidiol (CBD) Compound; NBC News, ABC News and Huffington Post Report California Pacific Medical Center’s Findings That CBD Stops Metastasis in Aggressive Cancers – The Wall Street Journal

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“Medical Marijuana Inc Announces Positive Developments in Recent Studies Using Cannabidiol (CBD) Compound; NBC News, ABC News and Huffington Post Report California Pacific Medical Center’s Findings That CBD Stops Metastasis in Aggressive Cancers

SAN DIEGO, May 28, 2013 (GLOBE NEWSWIRE) — Medical Marijuana Inc (OTC Pink:MJNA) is pleased to inform shareholders and the general public of recent developments in the research involving Cannabidiol (CBD) and other Phyto-cannabinoids.

The Following is taken from a Huffington Post interview with Dr. McAllister and Dr. Desprez:

A pair of scientists at California Pacific Medical Center in San Francisco has found that a compound derived from marijuana could stop metastasis in many kinds of aggressive cancer, potentially altering the fatality of the disease forever.

“It took us about 20 years of research to figure this out, but we are very excited,” said Pierre Desprez, one of the scientists behind the discovery, to The Huffington Post. “We want to get started with trials as soon as possible.”

The Daily Beast first reported on the finding, which has already undergone both laboratory and animal testing, and is awaiting permission for clinical trials in humans.

Desprez, a molecular biologist, spent decades studying ID-1, the gene that causes cancer to spread. Meanwhile, fellow researcher Sean McAllister was studying the effects of Cannabidiol, or CBD, a non-toxic, non-psychoactive chemical compound found in the cannabis plant. Finally, the pair collaborated, combining CBD and cells containing high levels of ID-1 in a petri dish.

“What we found was that his Cannabidiol could essentially ‘turn off’ the ID-1,” Desprez told HuffPost. The cells stopped spreading and returned to normal.

“We likely would not have found this on our own,” he added. “That’s why collaboration is so essential to scientific discovery.”

Desprez and McAllister first published a paper about the finding in 2007. Since then, their team has found that CBD works both in the lab and in animals. And now, they’ve found even more good news.

“We started by researching breast cancer,” said Desprez. “But now we’ve found that Cannabidiol works with many kinds of aggressive cancers–brain, prostate–any kind in which these high levels of ID-1 are present.”

Desprez hopes that clinical trials will begin immediately.

“We’ve found no toxicity in the animals we’ve tested, and Cannabidiol is already used in humans for a variety of other ailments,” he said. Indeed, the compound is used to relieve anxiety and nausea, and, since it is non-psychoactive, does not cause the “high” associated with THC.

While marijuana advocates will surely praise the discovery, Desprez explained that it’s not so easy as just lighting up.

“We used injections in the animal testing and are also testing pills,” he said. “But you could never get enough Cannabidiol for it to be effective just from smoking.”

Additional Information:

Dr. McAllister & CBD Research

Dr. Sean McAllister says that he is ready to begin testing CBD on humans to evaluate anti-cancer properties. Dr. McAllister and colleague Pierre Desprez, PhD from California Pacific Medical Center have previously mentioned, “Cannabidiol offers hope of a non-toxic therapy that could treat aggressive forms of cancer without any of the painful side effects of chemotherapy.” “We found that this one compound, CBD, had a specific effect on metastatic cancer cells, very aggressive tumor cells. CBD in animal studies has been used to ‘switch off’ a specific gene regulator.” Dr. McAllister explains: “We find when you treat with CBD, you down regulate the expression of this protein and that inhibits the disease process.” Dr. McAllister and Dr. Desprez have developed a synthetic version of CBD, which they say targets a specific gene in the body related to the spread of cancer (metastasis). Article: http://abclocal.go.com/kgo/story?section=news/health&id=9057615

Additional Cannabidiol Information

ABC News-

http://abclocal.go.com/kgo/story?section=news/health&id=9057615

Huffington Post-

http://www.huffingtonpost.com/2012/09/19/marijuana-and-cancer_n_1898208. html?ncid=edlinkusaolp00000003&ir=Weird%20News

US. National Cancer Institute

http://www.cancer.gov/cancertopics/pdq/cam/cannabis/healthprofessional/p age4

Additional Dr. McAllister Publications

http://www.ncbi.nlm.nih.gov/pubmed/?term=Sean%20McAllister

Additional Published Material on Cannabidiol (CBD)

http://www.ncbi.nlm.nih.gov/gquery/?term=CANNABIDIOL”

More: http://online.wsj.com/article/PR-CO-20130528-906109.html

Bay Area Researchers Claim Cannabis Can Cure Cancer

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“Marijuana has been used for medicinal purposes–relieving stress and pain and fighting hunger and nausea–for centuries if not millennia. But now, a pair of doctors in San Francisco claim that they’ve compiled reliable data showing that a certain compound in cannabis–cannabidiol–may actually cure cancer.”

Bay Area Researchers Claim Cannabis Can Cure Cancer

“Unlike THC, the ingredient in marijuana that makes you feel stoned, cannabidiol is a non-toxic compound of the plant that has no psychoactive qualities, and it’s been the focus of an ongoing series of trials at the San Francisco-based California Pacific Medical Center. There, physicians Sean McAllister and Pierre Desprez claim they’ve successfully used cannabidiol to fight animal genes involved in the spread of cancer. Now they hope to be allowed to conduct anti-cancer research using cannabidiol on actual humans.”

Cannabidiol reduces cigarette consumption in tobacco smokers: Preliminary findings.

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“The role of the endocannabinoid system in nicotine addiction is being increasingly acknowledged. We conducted a pilot, randomised double blind placebo controlled study set out to assess the impact of the ad-hoc use of cannabidiol (CBD) in smokers who wished to stop smoking.

24 smokers were randomised to receive an inhaler of CBD (n=12) or placebo (n=12) for one week, they were instructed to use the inhaler when they felt the urge to smoke.

 Over the treatment week, placebo treated smokers showed no differences in number of cigarettes smoked.

In contrast, those treated with CBD significantly reduced the number of cigarettes smoked by ~40% during treatment.

 Results also indicated some maintenance of this effect at follow-up.

 These preliminary data, combined with the strong preclinical rationale for use of this compound, suggest CBD to be a potential treatment for nicotine addiction that warrants further exploration.”

http://www.ncbi.nlm.nih.gov/pubmed/23685330