Tag Archives: CB(1) and CB(2) receptors

Therapeutic Potential of Cannabinoids in Schizophrenia.

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“Increasing evidence suggests a close relationship between the endocannabinoid system and schizophrenia.

The endocannabinoid system comprises of two G protein-coupled receptors (the cannabinoid receptors 1 and 2 [CB1 and CB2] for marijuana’s psychoactive principle Δ9-tetrahydrocannabinol), their endogenous small lipid ligands (namely anandamide [AEA] and 2-arachidonoylglycerol [2-AG], also known as endocannabinoids), and proteins for endocannabinoid biosynthesis and degradation.

…antipsychotic compounds which manipulate this system may provide a novel therapeutic target for the treatment of schizophrenia.

The present article reviews current available knowledge on herbal, synthetic and endogenous cannabinoids with respect to the modulation of schizophrenic symptomatology.

Furthermore, this review will be highlighting the therapeutic potential of cannabinoid-related compounds and presenting some promising patents targeting potential treatment options for schizophrenia.”

http://www.ncbi.nlm.nih.gov/pubmed/24605939

Combining rimonabant and fentanyl in a single entity: preparation and pharmacological results.

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“Based on numerous pharmacological studies that have revealed an interaction between cannabinoid and opioid systems at the molecular, neurochemical, and behavioral levels, a new series of hybrid molecules has been prepared by coupling the molecular features of two wellknown drugs, ie, rimonabant and fentanyl. The new compounds have been tested for their affinity and functionality regarding CB1 and CB2 cannabinoid and μ opioid receptors. In [(35)S]-GTPγS (guanosine 5′-O-[gamma-thio]triphosphate) binding assays from the post-mortem human frontal cortex, they proved to be CB1 cannabinoid antagonists and μ opioid antagonists. Interestingly, in vivo, the new compounds exhibited a significant dual antagonist action on the endocannabinoid and opioid systems.”

http://www.ncbi.nlm.nih.gov/pubmed/24591816

Cannabinoid CB1 Receptor Is Downregulated in Clear Cell Renal Cell Carcinoma

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“Several studies in cell cultures and in animal models have demonstrated that cannabinoids have important antitumoral properties… many of these effects are mediated through cannabinoid (CB) receptors CB1 and CB2…

The obtained data suggest a possible implication of the endocannabinoid system in renal carcinogenesis.”

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2989249/

 

 

Cannabinoid CB1 receptor is expressed in chromophobe renal cell carcinoma and renal oncocytoma.

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“Objective: To analyze the mRNA and protein expression of cannabinoid receptors CB1 and CB2 in chromophobe renal cell carcinoma (ChRCC) and renal oncocytoma (RO)…

RESULTS:

Quantitative RT-PCR analysis showed that CB1 mRNA was underexpressed by 12-fold in ChRCC and had a variable expression in RO. CB1 protein showed intense positive immunostaining in both neoplasms. Both CB2 mRNA and protein were not expressed in tumor and non tumorrenal tissue.

CONCLUSION:

This distinct immunoprofile may eventually be used as an additional tool with practical interest in the differential diagnosis of renal tumors.”

http://www.ncbi.nlm.nih.gov/pubmed/23318578

The peripheral cannabinoid receptor: adenylate cyclase inhibition and G protein coupling.

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“Two cannabinoid receptors, designated neuronal (or CB1) and peripheral (or CB2), have recently been cloned. Activation of CB1 receptors leads to inhibition of adenylate cyclase and N-type voltage-dependent Ca2+ channels.

Here we show, using a CB2 transfected Chinese hamster ovary cell line, that this receptor binds a variety of tricyclic cannabinoid ligands as well as the endogenous ligand anandamide.

Activation of the CB2 receptor by various tricyclic cannabinoids inhibits adenylate cyclase activity and this inhibition is pertussis toxin sensitive indicating that this receptor is coupled to the Gi/G(o) GTP-binding proteins…

These results characterize the CB2 receptor as a functional and distinctive member of the cannabinoid receptor family.”

http://www.ncbi.nlm.nih.gov/pubmed/7498464

 

Potential protective effects of cannabidiol on neuroanatomical alterations in cannabis users and psychosis: a critical review.

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“…different cannabis compounds may exert opposite effects on the neuroanatomical changes underlying psychosis. In particular, cannabidiol (CBD) was shown to prevent THC associated hippocampal volume loss… This finding is further supported by several animal experiments supporting neuroprotective properties of CBD mainly via anti-oxidative effects, CB2 receptors or adenosine receptors… mechanisms by which CBD may reduce brain volume loss, including antagonism of THC, interactions with endocannabinoids, and mechanisms that specifically underlie antipsychotic properties of CBD.”

http://www.ncbi.nlm.nih.gov/pubmed/22716143

(+)-Cannabidiol analogues which bind cannabinoid receptors but exert peripheral activity only.

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“We have tested a series of (+)-cannabidiol derivatives… for central and peripheral (intestinal, antiinflammatory and peripheral pain) effects in mice…

We conclude that centrally inactive (+)-cannabidiol analogues should be further developed as antidiarrheal, antiinflammatory and analgesic drugs for gastrointestinal and other peripheral conditions.”

http://www.ncbi.nlm.nih.gov/pubmed/15588739

Peripheral, but not central effects of cannabidiol derivatives: mediation by CB(1) and unidentified receptors.

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“Delta-9 tetrahydrocannabinol (Delta(9)-THC) and (-)-cannabidiol ((-)-CBD) are major constituents of the Cannabis sativa plant with different pharmacological profiles…

We tested a series of (+)- and (-)-CBD derivatives for central and peripheral effects in mice…

We suggest that (+)-CBD analogues have mixed agonist/antagonist activity in the brain.

Second, (-)-CBD analogues which are devoid of cannabinoid receptor affinity but which inhibit intestinal motility, suggest the existence of a non-CB(1), non-CB(2) receptor.

Therefore, such analogues should be further developed as antidiarrheal and/or antiinflammatory drugs.

We propose to study the therapeutic potential of (-)- and (+)-CBD derivatives for complex conditions such as inflammatory bowel disease and cystic fibrosis.”

http://www.ncbi.nlm.nih.gov/pubmed/15910887

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