NUCLEAR STRENGTH CANNABINOIDS - THE LAST RESORT?

NUCLEAR STRENGTH CANNABINOIDS - THE LAST RESORT?

HU-210 Kills Cancer Cells in Many Trials

 

"The synthetic cannabinoid HU-210 might cure some forms of cancer, kick start stem cells into regenerating nerve and other cells, and more, but there might be dangerous overtones...."  - MMJDoctorOnline

 

This article contains takeaway information about the most studied synthetic cannabinoid, HU-210. The information is applicable to both laymen and physicians alike and provide a comprehensive list of research studies that attest to the potential, efficacy and dangers of this very powerful cannabinoid.  Unfortunately, HU-210 is unavailable for prescription at this point, but many researchers believe that megadosing THC may achieve similar results.  

 

Nuclear Cannabinoids

 

So, what exactly is HU-210?

HU-210 is a psychoactive synthetic cannabinoid that acts somewhat like THC except it is much stronger. Though HU-210 is not normally found in Spice, a dangerous illegal mix of synthetic cannabinoid due to its poor smokability.  While Cannabinoids found in cannabis can be titrated at home, no one should mess about with HU-210 without a doctor's prescription and supervision.  A doctor's recommendation for medical marijuana does not entitle patients to buy or use HU-210, because it is not a marijuana component.  HU-210 is a pharmaceutical, plain and simple and is not allowed under prescription as a schedule I drug.

HU-210 first synthesized in 1988 at Hebrew University by a group led by Professor Raphael Mechoulam. Dr. Mechoulam was also Cannabis.  HU-210 was subsequently found to be 100 to 800 times more potent !!! than natural THC with an extended duration of activity. The "HU" stands for Hebrew University. 

 

"Evidence is emerging to suggest that cannabinoids are potent inhibitors of both cancer growth and spreading. Because cannabinoids are usually well tolerated and do not develop the toxic effects of conventional chemotherapeutics, more preclinical studies are warranted to investigate a potential utility of these substances as anticancer therapeutics."

 

Clinical and Scientific studies strongly suggest of find that HU-210

 
  • Increases blood supply and protects against hypothermia by binding to CB1 receptors, which influence cardiovascular function.
  • Protests against ischemic damage, the restriction in blood supply to tissues, resulting in a shortage of oxygen and glucose.
  • Neuroprotection results from the mirror image of HU-210 molecule, called HU-211 has very similar cannabinoid activity, except it acts as an antagonist (dials down receptor activity.
  • HU-210 promotes rapid cellular reproduction , but not differentiation, of cultured neural stem cells.
  • Increased neural growth led to antianxiety and antidepressant effects.
  • HU-210 is a potent pain killer similar to but more powerful than THC.
 
 

HU-210 molecule

  • HU - 210 Molecule - Slight differences in structure(compared to THC) amplify biochemical effects by 100 or more times.  
  • HU-210 was found to prevent inflammation found in Alzheimer's disease; stopped production of amyloid beta proteins.
  • HU-210 reduced cognitive impairment and loss of neuronal markers in Alzheimer's.
  • Cannabinoids including HU-210 completely negated neurotoxicity in rats.
  • HU-210 is a schedule I controlled substance under the CSA.   The drug or other substance has a high potential for abuse ;substance has no currently accepted medical use in treatment in the United States; there is a lack of accepted safety for use of the drug or other substance under medical supervision.

 

One little bond makes all the difference - HU-211

 
 

HU-211 - Nontoxic?  Brain Cancer Treatment?

The mirror image molecule of HU-210, Dexanabinol (HU-211) Unlike other cannabinoid derivatives, HU-211 does not act as a cannabinoid receptor agonist (activator) but instead has antagonist (dials down) effects and does not produce cannabis-like effects, However HU-211 demonstrates anticonvulsant and neuroprotective effects which imply efficacy in treating head injury, stroke, or cancer.   HU-211 was shown to be safe in clinical trials  and is currently studied in clinical trials for the treatment of brain cancer and advanced solid tumors.

Conclusion:  HU-210 study and application might best be focused on extremely difficult to treat and advanced and otherwise untreatable conditions; namely cancer, massive neurological damage and stem cell therapy.

 

MMJDoctorOnline Notes:  A 420 Recommendation will not allow you to buy HU-210.  However, it does allow you to select from a vast array of cannabis based medicines from licenses suppliers in both California and Nevada.  Fortunately the Medical Board of California approves of patients applying online to get a physician's evaluation for medical cannabis, Marijuana ID Card and also grower's permit.  We have made this process as simple and affordable as possible - its 100% online- takes a few minutes and your file is processed same day.  Our MMJ documents are accepted by Cannabis Dispensaries, Compasion Clubs, Licensed Delivery Services, Online Suppliers, cooperatives and clinics in both California and Nevada.

 

affinity of receptors for cannabinoids

 
 

RESEARCH STUDIES AND CLINICAL TRIALS

 

Material Safety Data Sheet - HU-210

Cannabinoids: a real prospect for pain relief

Recent advances include evidence that cannabinoid agonists are antihyperalgesic and antiallodynic in models of neuropathic pain. Development of novel cannabinoid agonists and cannabinoid preparations that are antinociceptive has important implications for the therapeutic use of this class of drugs.

Attenuation the acute actions of the highly potent cannabinoid receptor agonist HU-210 on defensive-withdrawal behavior in rats.

Enhancement of anxiety-like responsiveness to the cannabinoid CB1 receptor agonist HU-210 following chronic stress

The effect that chronic unpredictable stress had on the anxiety-like response elicited by the cannabinoid receptor agonist HU-210 Results demonstrated that in unstressed animals, a low dose of HU-210 induced an anxiolytic (anti-anxiety) response, whereas a high dose induced an anxiety.

Marijuana-based Drugs: Innovative Therapeutics or Designer Drugs of Abuse?

Therapeutic doses of both CB1Receptor agonists and antagonists (dial up and dial down) can produce unacceptable psychiatric effects. Several strategies to mitigate side effects are being investigated...... We conclude that marijuana-based drugs are indeed worthy of future study and characterization, in order to rigorously investigate their pharmacodynamic and potential clinical effects.

Cannabinoids promote embryonic and adult hippocampus neurogenesis and produce anxiolytic- and antidepressant-like effects

Adult hippocampal neurogenesis (neurons generated from stem cells) is suppressed by chronic use of opiates, alcohol, nicotine, and cocaine. This study suggests that cannabinoids are the only illicit drug that promotes adult hippocampal neurogenesis following chronic administration. Increased hippocampal neurogenesis appears to underlie the mechanism .....may finally explain discrepancies in the clinical study literature regarding the effects of cannabinoid on anxiety and depression.

HU-210- a synthetic cannabinoid & Cannabis studies completed

Learning impairment produced in rats by the cannabinoid agonist HU 210 in a water-maze task.

HU 210 at 50 or 100 microg/kg (once daily for 4 days, 60 min before a daily session) impaired learning in the place version but not in the cue one; .... Motor activity was compromised by the same treatment schedule.

Suppression of Nerve Growth Factor Trk Receptors and Prolactin Receptors by Endocannabinoids Leads to Inhibition of Human Breast and Prostate Cancer Cell Proliferation

Anandamide and HU-210 exerted a strong inhibition of the levels of NGF Trk receptors ..... the proliferation of prostate DU-145 cells was potently inhibited ....

Involvement of central and peripheral cannabinoid receptors in the regulation of heart resistance to arrhythmogenic effects of epinephrine.

HU-210 is probably related to activation of type II peripheral cannabinoid receptors.

Inhibitory effects of the cannabinoid agonist HU 210 on rat sexual behaviour.

HU 210 (25-100 microg/kg, i.p.) inhibited female sexual behaviour, potently reducing lordosis quotient and lordosis intensity.

Targeting CB2 cannabinoid receptors as a novel therapy to treat malignant lymphoblastic disease

THC, HU-210, and anandamide induce apoptosis (cancer cell death) in human leukemia and lymphoma cell lines in vitro.

Influence of the CB1 receptor antagonist, AM 251, on the regional haemodynamic effects of WIN-55212-2 or HU 210 in conscious rats

There was still a substantial fall in blood pressure in response to HU 210 (−57 mm Hg) which was not accounted for either by a fall in cardiac output, or by peripheral vasodilatation. .... it seems that responses to HU 210 may be influenced substantially by anaesthesia.

Activation of cannabinoid receptors decreases the area of ischemic myocardial necrosis.

Results indicate that cannabinoid receptor agonist HU-210 possesses cardioprotective activity and delays the formation of necrotic zones during coronary occlusion and reperfusion.

Increase of the heart arrhythmogenic resistance and decrease of the myocardial necrosis zone during activation of cannabinoid receptors

We have found that intravenous administration of cannabinoid receptor (CB) agonist HU-210 (0.05 mg/kg), increases cardiac resistance against arrhythmogenic effect of epinephrine, aconitine, coronary artery occlusion and reperfusion in rats.

The cannabinoids R(-)-7-hydroxy-delta-6-tetra-hydrocannabinol-dimethylheptyl (HU-210), 2-O-arachidonoylglycerylether (HU-310) and arachidonyl-2-chloroethylamide (ACEA) increase isoflurane provoked sleep duration by activation of cannabinoids 1 (CB1)-receptors in mice.

We found that the CB receptor agonists ......significantly prolong the duration of isoflurane induced sleep in mice.

CB1 cannabinoid receptor antagonism promotes remodeling and cannabinoid treatment prevents endothelial dysfunction and hypotension in rats with myocardial infarction

HU-210 acutely elicits hypotension (lowers blood pressure) and bradycardia (lowers pulse rate)  via CB1 receptors.

Drug-induced hypothermia reduces ischemic damage: effects of the cannabinoid HU-210.

HU-210 confers robust protection against ischemic (oxygen starvation) damage. This protection is mediated at least in part by binding to CB1 receptors and is also associated with the indirect protective effects of hypothermia. (Stroke. 2003;34: 2000-2006.)

Histamine induced responses are attenuated by a cannabinoid receptor agonist in human skin.

In humans peripheral administration of a cannabinoid receptor agonist attenuates histamine-induced itch. .... alleviation of itch is not due to an anti-histaminergic property of HU210.

The endogenous cannabinoid system protects against colonic inflammation

The endogenous cannabinoid system is physiologically involved in the protection against excessive inflammation in the colon, both by dampening smooth muscular irritation caused by inflammation and by controlling cellular pathways leading to inflammatory responses. These results strongly suggest that modulation of the physiological activity of the endogenous cannabinoid system during colonic inflammation might be a promising therapeutic tool for the treatment of several diseases characterized by inflammation of the gastrointestinal tract.

Cannabinoids spell relief in colon inflammation

The treatment of wild-type mice with a THC-like substance (HU210) was able to strongly reduce the degree of inflammation.

Cannabinoids provide neuroprotection against 6-hydroxydopamine toxicity in vivo and in vitro: relevance to Parkinson's disease.

We found that the non-selective cannabinoid agonist HU-210 increased cell survival in cultures of mouse cerebellar granule cells exposed to this toxin.

Arthritis and cannabinoids: HU-210 and Win-55,212-2 prevent IL-1alpha-induced matrix degradation in bovine articular chondrocytes in-vitro.

The results showed that HU-210 significantly inhibited collagen degradation.

Cannabinoids Ameliorate Pain and Reduce Disease Pathology in Cerulein-Induced Acute Pancreatitis

In humans, acute pancreatitis is associated with ... receptors of the endocannabinoid system in the pancreas..... results suggest a therapeutic potential for cannabinoids in abolishing pain associated with acute pancreatitis and in partially reducing inflammation .....in the absence of adverse side effects.

Arthritis and cannabinoids: HU-210 and Win-55,212-2 prevent IL-1alpha-induced matrix degradation in bovine articular chondrocytes in-vitro.

Biologically stable synthetic cannabinoids protect cartilage matrix from degradation induced by cytokines and this effect is possibly CB-receptor mediated and involves effects on prostaglandin and nitric oxide metabolism. Cannabinoids could also be producing these effects via inhibition of NF-kappaB activation.

proteins - little biological robots that run errands

The wild molecules that proteins are, Interferon, which sent messages....

Increased endocannabinoid levels reduce the development of precancerous lesions in the mouse colon

Enhancement of colon endocannabinoid levels ...may be protective against preneoplastic lesions in the mouse colon; ..... This protective effect could be due to indirect activation of apoptosis of colon preneoplastic cells.

Cannabinoids Induce Glioma Stem-like Cell Differentiation and Inhibit Gliomagenesis

Cannabinoids are known to exert an antitumoral action against gliomas and a variety of tumors of different origins ...in addition to inducing apoptosis .... cannabinoids promote differentiation of GSCs and inhibit tumor initiation.....results demonstrate the action of cannabinoids on glioma stem-like cells and thus may open new avenues for cannabinoid-based antitumoral strategies.

The synthetic cannabinoid HU210 induces spatial memory deficits and suppresses hippocampal firing rate in rats

Spatial impairment may be due to HU210 causing a reduction of hippocampal neural excitation.

The synthetic cannabinoids attenuate allodynia and hyperalgesia in a rat model of trigeminal neuropathic pain.

Cannabinoids may be a useful therapeutic approach for the clinical management of trigeminal neuropathic pain disorders.

Excitotoxicity in a chronic model of multiple sclerosis: Neuroprotective effects of cannabinoids through CB1 and CB2 receptor activation.

These data underline the implication of excitotoxic (reducing damage through overactivation of neurons) processes in demyelinating (nerve fiber coating) pathologies such as MS and the potential therapeutic properties (by dialing down) of cannabinoids.

Repeated Cannabinoid Injections into the Rat Periaqueductal Gray Enhances Subsequent Morphine Antinociception

The present data showed no enhancement of motor inhibition produced by morphine in rats pretreated with HU-210, suggesting that HU-210 enhancement of morphine may be specific to antinociception.

Cannabinoid receptor 1 is a potential drug target for treatment of translocation-positive rhabdomyosarcoma

For the first time, results show that HU210 has tumor growth inhibiting properties in vivo. This could represent one possible novel treatment strategy that might improve outcome in this pediatric tumor.

Lipid rafts regulate 2-arachidonoylglycerol metabolism and physiological activity in the striatum

Both cholesterol and cannabinoid receptors in the pathophysiology of neurodegenerative disorders lipid raft-ECS interaction point to further investigation...

Involvement of cannabinoid-1 and cannabinoid-2 receptors in septic ileus.

Our findings for the first time suggest a role of CB1 and CB2 receptors in the pathophysiology of septic ileus - lack of movement in the intestines that leads to a buildup or blockage of food material...

Cannabis mechanism to kill cancer

Antitumorigenic Effects of Cannabinoids beyond Apoptosis

Evidence is emerging to suggest that cannabinoids are potent inhibitors of both cancer growth and spreading. Because cannabinoids are usually well tolerated and do not develop the toxic effects of conventional chemotherapeutics, more preclinical studies are warranted to investigate a potential utility of these substances as anticancer therapeutics.

Regulation of nausea and vomiting by cannabinoids

Preclinical research indicates that cannabinioids, including CBD, may be effective clinically for treating both nausea and vomiting produced by chemotherapy or other therapeutic treatments.

Now, There's a Test for That -- Norchem's "Fake Marijuana" Test Reveals Significantly Increased Abuse of Spice/K2

We consider teenage and college age groups most at risk,..... standard screening for street drugs will not detect Spice/K2. But it's a quickly growing problem, and we encourage law enforcement, drug courts, probation and social services agencies to request testing. They may be shocked to see the abuse levels in these drugs.

The potential for clinical use of cannabinoids in treatment of cardiovascular diseases.

The evidence of a potential role for cannabinoid in various cardiovascular pathologies,.... HU210 has a proven safety profile in humans and given its favorable myocardial protection properties should be tested in humans.

Beyond THC: The New Generation of Cannabinoid Designer Drugs.

Importantly, understanding of the neurobiological bases of such compounds activity might encourage the development of synthetic cannabinoids that produce therapeutic effects with a minimum of psychoactive effects, such as the synthetic THC dronabinol (Marinol), the synthetic THC analog nabilone (Cesamet), and the standardized cannabis extract (Sativex).

Investigating a not-so-natural high.

Further analysis at the CBP laboratory in Chicago confirmed the presence of HU-210..... CBP seized >100 lb of HU-210-laced herbal mixtures in five separate shipments...... a narcotics detector dog led authorities to the substance ....).

Pharmacological activation/inhibition of the cannabinoid system affects alcohol withdrawal-induced neuronal hypersensitivity to excitotoxic insults.

The stimulation of the endocannabinoid system is protective against the hyperexcitability developed during alcohol withdrawal. By contrast, the blockade of the endocannabinoid system is highly counterproductive during alcohol withdrawal.

Regulation of nausea and vomiting by cannabinoids.

Preclinical research indicates that cannabinioids, including CBD, may be effective clinically for treating both nausea and vomiting produced by chemotherapy or other therapeutic treatments.

Cannabinoid Receptor Type 1 Protects Nigrostriatal Dopaminergic Neurons against MPTP Neurotoxicity by Inhibiting Microglial Activation

The present in vivo and in vitro findings clearly indicate that the CB1 receptor possesses anti-inflammatory properties and inhibits microglia-mediated oxidative stress. ....is beneficial for the treatment of Parkinson’s disease and other disorders associated with neuroinflammation and microglia-derived oxidative damage.

The effects of cannabinoid drugs on abnormal involuntary movements in dyskinetic and non-dyskinetic 6-hydroxydopamine lesioned rats.

Finding suggest that endocannabinoid tone (cannabinoid replacement therapy) may confer protection against the development of levodopa-induced dyskinesias (motor skill dysfunction caused by LDopa).

Increased brain metabolism after acute administration of the synthetic cannabinoid HU210: A small animal PET imaging study with (18)F-FDG.

HU210 increases brain glucose metabolism in the rat brain shortly after administration, in line with normalised human in vivo studies....

Contrasting effects of different cannabinoid receptor ligands on mouse ingestive behavior.

The potent and nonselective CB1 receptor agonist HU-210 and the selective CB1 receptor agonists .......The CB1 receptor antagonist rimonabant produced effects that were opposite in direction to those produced by Δ9-THC.

Long-term use of HU210 adversely affects spermatogenesis in rats by modulating the endocannabinoid system.

HU210, a selective agonist for CB1 and CB2 cannabinoid receptors impairs spermatogenesis and sperm motility and deregulates the endocannabinoid system.

Simultaneous analysis of several synthetic cannabinoids, THC, CBD and CBN, in hair by ultra-high performance liquid chromatography tandem mass spectrometry. Method validation and application to real samples.

The method was successfully applied to the analysis of 179 real samples collected of consumers of Cannabis ....14 were found positive to at least one synthetic cannabinoid.

The spice in France: mixed herbs containing synthetic cannabinoids.

Europe has taken legal actions to ban or otherwise control Spice products and related compounds.
 

Analgesic effects of cannabinoids on central pain syndrome.

The intensity of analgesic (pain killing) actions of cannabinoids on the central pain syndrome in rats .....: HU-210 > WIN 55,212-2 > anandamide.

 
 
 
 
 
 
 
 
 

Labels: cancer HU210 Spice THC regeneration synthetic cannabinoid schedule 1

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