Tag Archives: cannabinoid

Cannabidiol promotes browning in 3T3-L1 adipocytes.

Posted on by

“Recruitment of the brown-like phenotype in white adipocytes (browning) and activation of existing brown adipocytes are currently being investigated as a means to combat obesity.

The present study was designed to investigate the effects of cannabidiol (CBD), a major nonpsychotropic phytocannabinoid of Cannabis sativa, on induction of browning in 3T3-L1 adipocytes.

These data suggest possible roles for CBD in browning of white adipocytes, augmentation of lipolysis, thermogenesis, and reduction of lipogenesis.

In conclusion, the current data suggest that CBD plays dual modulatory roles in the form of inducing the brown-like phenotype as well as promoting lipid metabolism.

Thus, CBD may be explored as a potentially promising therapeutic agent for the prevention of obesity.”

http://www.ncbi.nlm.nih.gov/pubmed/27067870

http://www.thctotalhealthcare.com/category/obesity-2/

Cannabinoid Receptors CB1 and CB2 Modulate the Electroretinographic Waves in Vervet Monkeys.

Posted on by

“The expression patterns of the cannabinoid receptor type 1 (CB1R) and the cannabinoid receptor type 2 (CB2R) are well documented in rodents and primates.

In vervet monkeys, CB1R is present in the retinal neurons (photoreceptors, horizontal cells, bipolar cells, amacrine cells, and ganglion cells) and CB2R is exclusively found in the retinal glia (Müller cells). However, the role of these cannabinoid receptors in normal primate retinal function remains elusive.

Using full-field electroretinography in adult vervet monkeys, we recorded changes in neural activity following the blockade of CB1R and CB2R by the intravitreal administration of their antagonists (AM251 and AM630, resp.) in photopic and scotopic conditions.

Our results show that AM251 increases the photopic a-wave amplitude at high flash intensities, whereas AM630 increases the amplitude of both the photopic a- and b-waves.In scotopic conditions, both blockers increased the b-wave amplitude but did not change the a-wave amplitude.

These findings suggest an important role of CB1R and CB2R in primate retinal function.”

http://www.ncbi.nlm.nih.gov/pubmed/27069692

MAPPING CANNABINOID RECEPTOR 1 ALLOSTERIC SITE(S): CRITICAL MOLECULAR DETERMINANT AND SIGNALING PROFILE OF GAT100 – A NOVEL, POTENT AND IRREVERSIBLY BINDING PROBE.

Posted on by

“One of the most abundant G-protein coupled receptors (GPCRs) in brain, the cannabinoid 1 receptor (CB1R) is a tractable therapeutic target for treating diverse psychobehavioral and somatic disorders.

Adverse on-target effects associated with small-molecule CB1R orthosteric agonists and inverse agonists/antagonists have plagued their translational potential. Allosteric CB1R modulators offer a potentially safer modality through which CB1R signaling may be directed for therapeutic benefit.

Rational design of candidate, drug-like CB1R allosteric modulators requires greater understanding of the architecture of the CB1R allosteric endodomain(s) and the capacity of CB1R allosteric ligands to tune the receptor’s information output.

These data help inform the engineering of newer-generation, druggable CB1R allosteric modulators and demonstrate the utility of GAT100 as a covalent probe for mapping structure-function correlates characteristic of the druggable CB1R allosteric space.”

http://www.ncbi.nlm.nih.gov/pubmed/27046127

Cannabis and cancer: toward a new understanding

Posted on by

Logo of curroncol

“The treatment of cancer, including the disease itself and the symptoms associated with cancer and its therapy, is one of the most important emerging frontiers in cannabinoid therapeutics.

This Current Oncology supplement brings together the work of some of the leading minds around the world who have dedicated themselves and their laboratories to understanding the role of cannabis and cannabinoids in the pathophysiology and management of cancer.

It is an unfortunate reality of 2016 that many doctors still lack the basic knowledge about cannabis, cannabinoids, and the endocannabinoid system that would enable them to have an informed discussion with their patients, and that the knowledge gap gives rise to stigmatization, alienation, and a fracture of the doctor–patient relationship.

Our patient describes her experience in trying to find answers and assistance, and with the help of her treating oncologist, she succeeds in securing legal access to cannabinoids, with remarkable results. Stories of this kind are occurring too often to be ignored or written off as placebo responses or outliers. As a medical profession, we are duty-bound to follow up on such experiences with critical and balanced investigation.”

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4791146/

In vitro and in vivo efficacy of non-psychoactive cannabidiol in neuroblastoma.

Posted on by

“Neuroblastoma (nbl) is one of the most common solid cancers in children. Prognosis in advanced nbl is still poor despite aggressive multimodality therapy. Furthermore, survivors experience severe long-term multi-organ sequelae. Hence, the identification of new therapeutic strategies is of utmost importance.

Cannabinoids and their derivatives have been used for years in folk medicine and later in the field of palliative care. Recently, they were found to show pharmacologic activity in cancer, including cytostatic, apoptotic, and antiangiogenic effects.

We investigated, in vitro and in vivo, the anti-nbl effect of the most active compounds in Cannabis, Δ(9)-tetrahydrocannabinol (thc) and cannabidiol (cbd)…

Both compounds have antitumourigenic activity in vitro and impeded the growth of tumour xenografts in vivo. Of the two cannabinoids tested, cbd was the more active. Treatment with cbd reduced the viability and invasiveness of treated tumour cells in vitro and induced apoptosis. Moreover, cbd elicited an increase in activated caspase 3 in treated cells and tumour xenografts.

 

Our results demonstrate the antitumourigenic action of cbd on nbl cells. Because cbd is a nonpsychoactive cannabinoid that appears to be devoid of side effects, our results support its exploitation as an effective anticancer drug in the management of nbl.”

http://www.ncbi.nlm.nih.gov/pubmed/27022310

“Neuroblastomas are cancers that start in early nerve cells (called neuroblasts) of the sympathetic nervous system, so they can be found anywhere along this system.”  http://www.cancer.org/cancer/neuroblastoma/detailedguide/neuroblastoma-what-is-neuroblastoma

The role of carbon monoxide on the anti-nociceptive effects and expression of cannabinoid 2 receptors during painful diabetic neuropathy in mice.

Posted on by

“The activation of cannabinoid 2 receptors (CB2R) attenuates chronic pain, but the role played by carbon monoxide synthesized by the inducible heme oxygenase 1 (HO-1) on the anti-nociceptive effects produced by a selective CB2R agonist, JWH-015, during painful diabetic neuropathy remains unknown.

The activation of HO-1 enhanced the anti-nociceptive effects of JWH-015 in diabetic mice, suggesting that coadministration of JWH-015 with CORM-2 or CoPP might be an interesting approach for the treatment of painful diabetic neuropathy in mice.”

http://www.ncbi.nlm.nih.gov/pubmed/27020787

Encapsulation of cannabinoid drugs in nanostructured lipid carriers.

Posted on by

“This study describes the development and optimization of a method to encapsulate the potent and expensive cannabinoids drugs in nanostructured lipid carriers; namely, URB597, AM251 and rimonabant have been considered. NLC production by melt and ultrasonication protocol has been specifically designed to optimize nanoparticle recovery and drug encapsulation efficiency. Special care has been devoted to the modality of oil and water phase emulsification and the entire production has been studied and discussed. NLC recovery, morphology, dimensional distribution and encapsulation efficiency are presented.”

http://www.ncbi.nlm.nih.gov/pubmed/26952905

Effects of cannabinoid receptor activation by CP55,940 on normal bladder function and irritation-induced bladder overactivity in non-awake anaesthetised rats.

Posted on by

“CP55,940 is a synthetic analogue of tetrahydrocannabidiol, which is a psychoactive ingredient of the Cannabis plant.

This study was designed to evaluate the effects of CP55,940 on normal bladder function in vivo and examine whether it suppresses urinary frequency induced by nociceptive stimuli in the bladder.

CP55,940 decreases bladder activity and urinary frequency induced by nociceptive stimuli, probably by suppression of bladder afferent activity. Effects of CP55,940 were abolished by both CBR antagonists. This data implicates a role for the endocannabinoid system in bladder mechanoafferent function in rats. In addition, our results show that CP55,940 reverses urinary frequency exemplified in an overactive bladder model, suggesting it could be an effective treatment for patients with lower urinary tract symptoms.”

http://www.ncbi.nlm.nih.gov/pubmed/26942594

Nabilone for the Management of Pain.

Posted on by

“Nabilone, a synthetic cannabinoid, is approved in many countries including, but not limited to, Canada, the United States, Mexico, and the United Kingdom for the treatment of severe nausea and vomiting associated with chemotherapy. Clinical evidence is emerging for its use in managing pain conditions with different etiologies. We review the efficacy and safety of nabilone for various types of pain as well as its abuse potential, precautions and contraindications, and drug interactions; summarize pertinent clinical practice guidelines; and provide recommendations for dosing, monitoring, and patient education.

Nabilone was most commonly used as adjunctive therapy and led to small but significant reductions in pain. The most common adverse drug reactions included euphoria, drowsiness, and dizziness. Nabilone was rarely associated with severe adverse drug reactions requiring drug discontinuation, and the likelihood of abuse was thought to be low. Although the optimal role of nabilone in the management of pain is yet to be determined, certain clinical practice guidelines consider nabilone as a third-line agent.”

http://www.ncbi.nlm.nih.gov/pubmed/26923810

Cannabinoid CB2 receptors are involved in the regulation of fibrogenesis during skin wound repair in mice.

Posted on by

“Studies have shown that cannabinoid CB2 receptors are involved in wound repair, however, its physiological roles in fibrogenesis remain to be elucidated.

In the present study, the capacity of cannabinoid CB2 receptors in the regulation of skin fibrogenesis during skin wound healing was investigated.

These results indicated that cannabinoid CB2 receptors modulate fibrogenesis and the TGF‑β/Smad profibrotic signaling pathway during skin wound repair in the mouse.”

http://www.ncbi.nlm.nih.gov/pubmed/26935001