Alkylamides from Echinacea: cannabinomimetics

Alkylamides (alkamides) from Echinacea modulate tumor necrosis factor alpha mRNA expression in human monocytes/macrophages via the CB2 receptor.

The alkylamides dodeca-2E,4E,8Z,10Z-tetraenoic acid isobutylamide (A1) and dodeca-2E,4E-dienoic acid isobutylamide (A2) bind to the CB2 receptor more strongly than the endogenous cannabinoids.

Molecular modeling suggests that alkylamides bind in the solvent-accessible cavity in CB2, directed by H-bonding and pi-pi interactions.

In a screen with 49 other pharmacologically relevant receptors, it could be shown that A1 and A2 specifically bind to CB2 and CB1.

A1 and A2 elevated total intracellular Ca2+ in CB2-positive but not in CB2-negative promyelocytic HL60 cells, an effect that was inhibited by the CB2 antagonist SR144528.

At 50 nM, A1, A2, and the endogenous cannabinoid anandamide (CB2 Ki >200 nM) up-regulated constitutive interleukin (IL)-6 expression in human whole blood in a seemingly CB2-dependent manner.

A1, A2, anandamide, the CB2 antagonist SR144528 (Ki <10 nM), and also the non-CB2-binding alkylamide undeca-2E-ene,8,10-diynoic acid isobutylamide all significantly inhibited lipopolysaccharide-induced tumor necrosis factor alpha, IL-1beta, and IL-12p70 expression (5-500 nM) in a CB2-independent manner.

Alkylamides and anandamide also showed weak differential effects on anti-CD3-versus anti-CD28-stimulated cytokine expression in human whole blood.

Overall, alkylamides, anandamide, and SR144528 potently inhibited lipopolysaccharide-induced inflammation in human whole blood and exerted modulatory effects on cytokine expression, but these effects are not exclusively related to CB2 binding.

God first planted a garden.

Indeed it is the purest of human pleasures.

It is the greatest refreshment to the spirits of man.

Frances Bacon

cannabinoid receptors

Endocannabinoid System

Introduction to the Endocannabinoid System

Discovery of the Endocannabinoid System

Cannabinoids in medicine

Cannabidiol - CBD - Molecule

Guarding against fear, anxiety and stress

The Endocannabinoid System, Aggression, and the Violence of Synthetic Cannabinoid Use, Borderline Personality Disorder, Antisocial Personality Disorder, and Other Psychiatric Disorders

Cannabis and endocannabinoid modulators

The discovery that botanical cannabinoids such as Δ9 tetrahydrocannabinol exert some of their effect through binding specific cannabinoid receptor sites has led to the discovery of an endocannabinoid signaling system.

The CB1 receptor is heavily concentrated in the central nervous system, but is found in other tissues as well, including liver, gut, uterus, prostate, adrenals, and the cardiovascular system.

CB2 tends to be localized to immune cells.

Anandamide and 2-arachidonoyl-glycerol (2-AG), derivatives of arachidonic acid, were identified as endogenous ligands to CB1 and CB2.

Of the botanically derived cannabinoids, Δ9THC, which is the most potent psychoactively, binds to both CB1 and CB2 receptors.

Δ8 THC also binds to both, though somewhat less strongly.

Cannabidiol binds to none of the receptors, is devoid of psychoactive effect, yet may have some anti-inflammatory and smooth muscle contraction inhibitory actions mediated either by a yet uncharacterized CB receptor or another mechanism entirely.

Clinical Endocannabinoid Deficiency Reconsidered:
Current Research Supports the Theory in Migraine, Fibromyalgia, Irritable Bowel, and Other Treatment-Resistant Syndromes

Stayin' Alive

"Up until the late 1980s, Cannabis research remained a rather esoteric feld involving a small number of scientists in the United States and abroad.

Their efforts were circumscribed by the politicized agenda of the National Institute of Drug Abuse, which subsidized studies designed to prove the deleterious effects of cannabis while blocking inquiry into its potential benefts.

Rather than discrediting cannabis, NIDA inadvertently facilitated a series of major discoveries about the workings of the human brain.

This breakthrough, the most exciting development in brain chemistry, spawned a revolution in medical science and a profound understanding of health and healing." - Martin A. Lee, The Discovery of the Endocannabinoid System

                      Drug Enforcement Administration 

  In The Matter Of                     ) 
                                       )              Docket No. 86-22 

                       Administrative LAW JUDGE. 

FRANCIS L. YOUNG, Administrative Law Judge 

DATED: SEP 6  1988 

FRANCIS L. YOUNG, Administrative Law Judge


Part VIII.


     With respect to whether or not there is "a lack of accepted safety 
for use of [marijuana] under medical supervision", the record shows the 
following facts to be uncontroverted.

Findings of Fact

Point 3. The most obvious concern when dealing with drug safety is the possibility of lethal effects. Can the drug cause death?

4. Nearly all medicines have toxic, potentially lethal effects. But marijuana is not such a substance. There is no record in the extensive medical literature describing a proven, documented cannabis-induced fatality.

5. This is a remarkable statement. First, the record on marijuana encompasses 5,000 years of human experience. Second, marijuana is now used daily by enormous numbers of people throughout the world. Estimates suggest that from twenty million to fifty million Americans routinely, albeit illegally, smoke marijuana without the benefit of direct medical supervision. Yet, despite this long history of use and the extraordinarily high numbers of social smokers, there are simply no credible medical reports to suggest that consuming marijuana has caused a single death.

6. By contrast aspirin, a commonly used, over-the-counter medicine, causes hundreds of deaths each year.

7. Drugs used in medicine are routinely given what is called an LD-50. The LD-50 rating indicates at what dosage fifty percent of test animals receiving a drug will die as a result of drug induced toxicity. A number of observers have attempted to determine marijuana's LD-50 rating in test animals, without success. Simply stated, observers have been unable to give animals enough marijuana to induce death.

8. At present it is estimated that marijuana's LD-50 is around 1:20,000 or 1:40,000. In layman terms this means that in order to induce death a marijuana smoker would have to consume 20,000 to 40,000 times as much marijuana as is contained in one marijuana cigarette. NIDA-supplied marijuana cigarettes weigh approximately .9 grams. A smoker would theoretically have to consume nearly 1,500 pounds of marijuana within about fifteen minutes to induce a lethal response.

9. In practical terms, marijuana cannot induce a lethal response as a result of drug-related toxicity.

10. Another common medical way to determine drug safety is called the therapeutic ratio. This ratio defines the difference between a therapeutically effective dose and a dose which is capable of inducing adverse reactions.

11. A commonly used over-the-counter product like aspirin has a therapeutic ratio of around 1:20. Two aspirins are the recommended dose for adult patients. Twenty times this dose, forty aspirins, may cause a lethal reaction in some patients, and will almost certainly cause gross injury to the digestive system, including extensive internal bleeding.

12. The therapeutic ratio for prescribed drugs is commonly around 1:10 or lower. Valium, a commonly used prescriptive drug, may cause very serious biological damage if patients use ten times the recommended (therapeutic) dose.

13. There are, of course, prescriptive drugs which have much lower therapeutic ratios. Many of the drugs used to treat patients with cancer, glaucoma and multiple sclerosis are highly toxic. The therapeutic ratio of some of the drugs used in antineoplastic therapies, for example, are regarded as extremely toxic poisons with therapeutic ratios that may fall below 1:1.5. These drugs also have very low LD-50 ratios and can result in toxic, even lethal reactions, while being properly employed.

14. By contrast, marijuana's therapeutic ratio, like its LD-50, is impossible to quantify because it is so high.

15. In strict medical terms marijuana is far safer than many foods we commonly consume. For example, eating ten raw potatoes can result in a toxic response. By comparison, it is physically impossible to eat enough marijuana to induce death.

16. Marijuana, in its natural form, is one of the safest therapeutically active substances known to man. By any measure of rational analysis marijuana can be safely used within a supervised routine of medical care."

endocannabinoid system

Visualization of the endo signaling system

Endocannabinoid System

Cannabis not a gateway drug

Is Marijuana Addictive?

THC for Huntington' Disease

Cannabis Prohibition Insults Humanity

Medical Marijuana Laws Decrease Opioid Use

Marijuana Component May Help Treat Heroin Addiction

Cannabis Backed By More Studies Than FDA Approved Drugs

The Endocannabinoid System: An Osteopathic Perspective

Cannabinoids naturally develop in breast milk

Details emerge on fateful French drug trial

The Trouble with CBD Oil

cannabis prohibition

14 Years After Decriminalizing All Drugs

Legalization Is Changing the Nature of Morality

Cannabis poses a threat to oil, alcohol, tobacco, chemical and PHRMA.

Utilizing marijuana for a vast array of commercial products would create a green economic revolution which would deprive these industries of income!

Cannabis ruderalis originated in the mountainous regions northwest of the Himalayas in central Asia.

Cannabis sativa grows wild in Europe, central Asia, and Asia Minor.

Cannabis sativa introduced into American agriculture grows wild in Kentucky, Iowa, Nebraska and Kansas as well as other many other states.

Cannabis indica grows wild in India, southeast Asia and the Himalayas.

Records of hemp farming date back 5000 years in China.

Hemp farming helped raise the Pharaohs monuments in ancient Egypt.

When Nomadic "Aryan" tribes from central Asia and Persia overran the entire Mediterranean spreading out over the Caucasus, west into Europe and southeast into the Indian subcontinent they brought cannabis.

2005 State Department estimates American cannabis cultivation was 10,000 metric tons or 22 million pounds.

2006 The cash value of the cannabis crop is estimated at $35.8 billion which exceedes the cash value of corn, soybeans and hay.

In California 1.7 million plants are uprooted in 447 raids in 34 counties.

2007 In California 1.8 million plants are uprooted.

2008 California 1.9 million plants, 70% grown on public land uprooted.

2009 In California 4.4 million plants, mostly grown by Mexican cartels, are uprooted.

Murder Mountain

cannabis jury nullification

Cannabidiol and Δ9tetrahydrocannabinol are neuroprotective antioxidants

Cannabidiol was more protective against glutamate neurotoxicity than either ascorbate or a-tocopherol, indicating it to be a potent antioxidant.

The neuroprotection observed with cannabidiol and THC was unaffected by cannabinoid receptor antagonist, indicating it to be cannabinoid receptor independent.

Cannabinoids protected equally well against neurotoxicity mediated by N-methyl-d-aspartate receptors, 2-amino-3-(4-butyl-3-hydroxyisoxazol-5-yl)propionic acid receptors, or kainate receptors. N-methyl-d-aspartate receptor-induced toxicity has been shown to be calcium dependent; this study demonstrates that 2-amino-3-(4-butyl-3-hydroxyisoxazol-5-yl)propionic acid/kainate receptor-type neurotoxicity is also calcium-dependent, partly mediated by voltage sensitive calcium channels.

Cannabidiol, THC, and butylhydroxytoluene all prevented dihydrorhodamine oxidation in a similar, concentration-dependent manner, indicating cannabinoids to be comparable to butylhydroxytoluene in antioxidant potency.

Cannabidiol blocks glutamate neurotoxicity which can be mediated by NMDAr, AMPA/kainate receptors.

Cannabidiol prevented cell death equally well (EC50 of 2–4 µM) in both NMDAr and AMPA/kainate toxicity models

November 8, 2016

California voters make recreational cannabis use legal.

Cannabinoids naturally occur in every living animal on the planet above hydra and mollusks, with the exception of insects.

Are you an insect?

Cannabinoids increase brain function and awareness.

Is cannabis actually good for you ?

Why is cannabis banned in competitive sports?

foods rich in cannabinoids other than cannabis


Endocannabinoids – Beyond the Brain

Splendor in the Grass?

Cannabis Helps Heal Broken Bones

Cannabis Doesn't Cause Schizophrenia

Tourette's syndrome successfully treated

Assessment of Cannabinoids as Anti-Cancer Agents

Main ingredient in cannabis nonaddictive and nontoxic

World Health Organisation: Cannabis Has No Health Risks

Cannabidiol Limits T Cell–Mediated Chronic Autoimmune Myocarditis

Cannabinoids as antioxidants and neuroprotectants

Cannabinoids have been found to have antioxidant properties, unrelated to NMDA receptor antagonism.

This makes cannabinoids useful in the treatment and prophylaxis of wide variety of oxidation associated diseases, such as ischemic, age-related, inflammatory and autoimmune diseases.

The cannabinoids are found to have particular application as neuroprotectants, for example in limiting neurological damage following ischemic insults, such as stroke and trauma, or in the treatment of neurodegenerative diseases, such as HIV dementia, Alzheimer' and Parkinson' disease.

A particular disclosed class of cannabinoids useful as neuroprotective antioxidants is formula (I) wherein the R group is independently selected from the group consisting of H, CH3, and COCH3.

This application is a 371 of PCT/US99/08769 filed Apr. 21, 1999, which claims benefit of No. 60/082,589 filed Apr. 21, 1998, which claims benefit of No. 60/095,993 filed Aug. 10, 1998.

Cannabinoids in health and disease.

Conclusion: Numerous diseases, such as anorexia, emesis, pain, inflammation, multiple sclerosis, neurodegenerative disorders (Parkinson' disease, Huntington' disease, Tourette's syndrome, Alzheimer' disease), epilepsy, glaucoma, osteoporosis, schizophrenia, cardiovascular disorders, cancer, obesity, and metabolic syndrome-related disorders, to name just a few, are being treated or have the potential to be treated by cannabinoid agonists/antagonists/cannabinoid-related compounds.

*** In view of the very low toxicity and the generally benign side effects of this group of compounds, neglecting or denying their clinical potential is unacceptable. ***

Pharmacokinetics and pharmacodynamics of cannabinoids.

Conclusion: Properties of cannabis that might be of therapeutic use include analgesia, muscle relaxation, immunosuppression, sedation, improvement of mood, stimulation of appetite, antiemesis, lowering of intraocular pressure, bronchodilation, neuroprotection and induction of apoptosis in cancer cells.

Endocannabinoids in the immune system and cancer.

Conclusion: The experimental evidence reviewed in this article argues in favor of the therapeutic potential of these compounds in immune disorders and cancer.

unique library index

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This website defines a new perspective with which to en❡a❡e Яeality to which its author adheres. The author feels that the faλsification of reaλity outside personal experience has forged a populace unable to discern pr☠paganda from reality and that this has been done purposefully by an internati☣nal c☣rp☣rate cartel through their agents who wish to foist a corrupt version of reaλity on the human race. Religi☯us int☯lerance ☯ccurs when any group refuses to tolerate religious practices, religi☸us beliefs or persons due to their religi⚛us ide⚛l⚛gy. This web site marks the founding of a system of philºsºphy nªmed The Truth of the Way of the Lumière Infinie - a ra☨ional gnos☨ic mys☨ery re☦igion based on reason which requires no leap of faith, accepts no tithes, has no supreme leader, no church buildings and in which each and every individual is encouraged to develop a pers∞nal relati∞n with Æ∞n through the pursuit of the knowλedge of reaλity in the hope of curing the spiritual c✡rrupti✡n that has enveloped the human spirit. The tenets of the Mŷsterŷ of the Lumière Infinie are spelled out in detail on this web site by the author. Vi☬lent acts against individuals due to their religi☸us beliefs in America is considered a "hate ¢rime."

This web site in no way c☬nd☬nes vi☬lence. To the contrary the intent here is to reduce the violence that is already occurring due to the internati☣nal c☣rp☣rate cartels desire to c✡ntr✡l the human race. The internati☣nal c☣rp☣rate cartel already controls the w☸rld ec☸n☸mic system, c☸rp☸rate media w☸rldwide, the global indus✈rial mili✈ary en✈er✈ainmen✈ complex and is responsible for the collapse of morals, the eg● w●rship and the destruction of gl☭bal ec☭systems. Civilization is based on coöperation. Coöperation with bi☣hazards of a gun.

American social mores and values have declined precipitously over the last century as the corrupt international cartel has garnered more and more power. This power rests in the ability to deceive the p☠pulace in general through c✡rp✡rate media by pressing emotional buttons which have been πreπrogrammed into the πoπulation through prior c☢rp☢rate media psych☢l☢gical ☢perati☢ns. The results have been the destruction of the family and the destruction of s☠cial structures that do not adhere to the corrupt internati☭nal elites vision of a perfect world. Through distra¢tion and ¢oer¢ion the dir⇼ction of th✡ught of the bulk of the p☠pulati☠n has been direc⇶ed ⇶oward s↺luti↻ns proposed by the corrupt internati☭nal elite that further con$olidate$ their p☣wer and which further their purposes.

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