Tag Archives: Cannabinoids

The anti-hyperalgesic actions of the cannabinoid anandamide and the putative CB2 receptor agonist palmitoylethanolamide in visceral and somatic inflammatory pain.

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“The therapeutic effects of the cannabinoid anandamide and the putative CB2 agonist palmitoylethanolamide were tested in a model of persistent visceral pain (turpentine inflammation of the urinary bladder)…

The results confirm the analgesic potential of endogenous ligands at cannabinoid receptor sites.

The anti-nociceptive effect of the putative CB2 receptor agonist, palmitoylethanolamide, is particularly interesting since it is believed to be a peripherally mediated effect.

This observation might be exploited to separate central psychotropic effects from peripheral analgesic actions of the cannabinoids, under inflammatory conditions.”

http://www.ncbi.nlm.nih.gov/pubmed/9696473

Cannabinoid receptor 2 is increased in acutely and chronically inflamed bladder of rats.

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“Cannabinoid receptors are expressed in the urinary bladder and may affect bladder function… CB2 receptors may be a viable target for pharmacological treatment of bladder inflammation and associated pain…

In this study, we have shown that CB1 and CB2 are present in the bladder and its innervation, and that expression of CB2 is increased in the bladders of rats with acute and chronic cystitis. Bladder inflammation and pain is the summation of a number of biological events, including participation of the endocannabinoid system.

The endocannabinoid system could play an important role in modulation of severity of bladder inflammation and pain, and it may be possible to take advantage of the cannabinoid system in the bladder to decrease inflammation and resultant pain.”

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2592089/

Increased cannabinoid receptor 1-immunoreactive nerve fibers in overactive and painful bladder disorders and their correlation with symptoms.

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“To study the expression of cannabinoid receptor 1 (CB1) in human urinary bladder hypersensitivity and overactivity disorders, and correlate changes with symptoms. Cannabinoid receptor agonists have been shown to modulate urinary bladder contractility and reduce pain after bladder inflammation; their clinical efficacy on lower urinary tract symptoms was demonstrated in the Cannabinoids in Multiple Sclerosis study…

CONCLUSIONS:

The results of this study suggest that increased nerve fibers, which express CB1, may be related to bladder pain in PBS (painful bladder syndrome) and urgency in IDO (idiopathic detrusor overactivity).

Our findings support clinical trials of CB1 agonists in bladder disorders.”

http://www.ncbi.nlm.nih.gov/pubmed/20346490

Differential expression of functional cannabinoid receptors in human bladder detrusor and urothelium.

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“Although cannabinoid receptor expression has been demonstrated in human brain and other peripheral neuronal tissues, definitive expression of these receptors in the human bladder has not been reported. Consequently we investigated the expression of functional cannabinoid 1 and 2 receptors in human bladder detrusor and urothelium…

CONCLUSIONS:

Together these findings suggest a physiological role of cannabinoid 1 and 2 receptors in the human bladder.

Moreover, these results confirm the presence of functional cannabinoid 1 and 2 receptors in the human bladder, which can serve as a target for drugs acting on symptoms of interstitial cystitis/painful bladder syndrome.”

http://www.ncbi.nlm.nih.gov/pubmed/19237176

Functional and immunohistochemical characterization of CB1 and CB2 receptors in rat bladder.

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“To determined the localization of CB(1) and CB(2) receptors in rat bladder and investigate the effect of a mixed CB(1)/CB(2) receptor agonist, ajulemic acid (AJA), on chemically evoked release of the sensory neuropeptide calcitonin gene-related peptide (CGRP)…

CONCLUSIONS:

CB(1) and CB(2) receptors are localized in the urothelium of rat bladder, and application of AJA inhibits the evoked release of CGRP by acting on CB(1) and CB(2) receptors.

These findings identify a potential new pathway for study in the evaluation and treatment of painful bladder syndrome/interstitial cystitis.”

http://www.ncbi.nlm.nih.gov/pubmed/18468662

Activation of cannabinoid receptor 2 inhibits experimental cystitis.

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“Cannabinoids have been shown to exert analgesic and anti-inflammatory effects, and the effects of cannabinoids are mediated primarily by cannabinoid receptors 1 and 2 (CB1and CB2). Both CB1 and CB2 are present in bladders of various species, including human, monkey, and rodents, and it appears that CB2 is highly expressed in urothelial cells…

The results of the current study indicate that CB2 is a potential therapeutic target for treatment of bladder inflammation and pain in patients.”

http://www.ncbi.nlm.nih.gov/pubmed/23515618

Targeting the Endocannabinoid System for Neuroprotection: A 19F-NMR Study of a Selective FAAH Inhibitor Binding with an Anandamide Carrier Protein, HSA.

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“Fatty acid amide hydrolase (FAAH), the enzyme involved in the inactivation of the endocannabinoid anandamide (AEA), is being considered as a therapeutic target for analgesia and neuroprotection…
The endocannabinoid system has been implicated as a therapeutic target for analgesia, anti-emesis, and neuroprotection… These findings provide a potential new therapeutic modality for neuroprotection through dual inhibition of FAAH and anandamide carrier proteins…”

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Updates in Reproduction Coming from the Endocannabinoid System.

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“The endocannabinoid system (ECS) is an evolutionarily conserved master system deeply involved in the central and local control of reproductive functions in both sexes. The tone of these lipid mediators-deeply modulated by the activity of biosynthetic and hydrolyzing machineries-regulates reproductive functions from gonadotropin discharge and steroid biosynthesis to the formation of high quality gametes and successful pregnancy.

This review provides an overview on ECS and reproduction and focuses on the insights in the regulation of endocannabinoid production by steroids, in the regulation of male reproductive activity, and in placentation and parturition.

Taken all together, evidences emerge that the activity of the ECS is crucial for procreation and may represent a target for the therapeutic exploitation of infertility.”

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3914453/

Changes in Cerebral CB1 Receptor Availability after Acute and Chronic Alcohol Abuse and Monitored Abstinence.

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“Involvement of the type 1 cannabinoid receptor (CB1R) in the effects of alcohol on the brain is supported by animal experiments…

In conclusion, whereas the acute alcohol effect is an increase in CB1R availability, chronic heavy drinking leads to reduced CB1R availability that is not reversible after 1 month of abstinence. Longer follow-up is required to differentiate whether this is a compensatory effect of repeated endocannabinoid overstimulation or an enduring trait-like feature.

An enhanced CB1R signaling may offer a new therapeutic direction for treatment of the negative affective state produced by alcohol withdrawal and abstinence, which is critical for the maintenance of alcohol addiction.”

http://www.ncbi.nlm.nih.gov/pubmed/24553924

Effects of Hemp (Cannabis sativa L.) Seed Oil Press-Cake and Decaffeinated Green Tea Leaves (Camellia sinensis) on Functional Characteristics of Gluten-Free Crackers.

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“A mixture, simplex centroid, 2 components experimental design was used to evaluate the addition of hemp seed oil press-cake and decaffeinated green tea leaves, as functional ingredients to assess nutritional characteristics and antioxidant properties of gluten-free crackers.

All samples with added hemp flour had much better nutritional qualities than the brown rice flour crackers in terms of higher protein, crude fibers, minerals, and essential fatty acids content. Likewise, all samples with added decaffeinated green tea leaves had much better antioxidant properties than crackers with no added green tea leaves. All crackers with added hemp flour had a significantly increased fiber content (39% to 249%) and decreased carbohydrate content (8.4% to 42.3%), compared to the brown rice flour crackers.

All samples had antioxidant properties, even without the addition of green tea leaves.

Optimization of the responses was conducted based on the maximized values for protein, fibers, omega-3 fatty acids content, as well as for the antioxidant activity and overall score. The suggested values for the addition of the hemp oil press-cake was 20% (total flour weight) with 4 g of decaffeinated green tea leaves that would provide protein content of 14.1 g/100 g; fibers content of 8.4 g/100 g; omega-3 fatty acids content of 3.2 g/100 g; antioxidant activity measured via 2,2-diphenyl-1-picrylhydrazyl value of 30.3 μmol TE/g d.w.; and an overall score of 8.9.

This formulation has demonstrated potential application in the baking industry and marketing of these gluten-free crackers as a value-added functional product.”

http://www.ncbi.nlm.nih.gov/pubmed/24527987