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Exciting New Cannabis Compound with Great Therapeutic Potential

Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor

Summary information:

A recent study has developed a synthetic compound that can act as an inverse agonist (a reverse activator) of cannabinoid receptor 1 (CB1.) Considering how prevalent these receptors are in the body, this may serve as a useful treatment for a great many concerns that involve this receptor, and/or for altering the effects of other cannabinoid therapies. The developed compounds are orally bioavailable and peripherally selective for CB1, meaning they can be taken by mouth and can still have action in the periphery of the body, as opposed to simply at the brain’s receptors. The selectivity and therapeutic benefits of these novel compounds present a promising development for the potential treatment of metabolic syndrome, diabetes, liver diseases, and gastrointestinal disorders, to name but a few.

Dr Caplan’s Input:

We have CB1 receptors from head-to-toe, through every organ, and just about everywhere in the body. This article highlights a few interesting points. While we have compounds which can activate a target cannabinoid receptor, the action in this review is actually stimulating an opposite impact (activating the opposite action, or an “inverse agonist” effect.) Also, the concept of targeting central (at the brain) vs peripheral (everywhere else) has not been well-addressed yet in Cannabis Medicine. If we can separate the two targets easily, the options for applications of cannabinoid therapies multiplies, as does the opportunity to eliminate undesirable effects.

View this review (yellow link) or download:

This paper is also stored here:   http://bit.ly/2UmvClo      inside the CED Foundation Archive

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Benjamin Caplan, MDExciting New Cannabis Compound with Great Therapeutic Potential
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Arizona Beverage Co embracing cannabis too

Arizona Beverage Co. has reached a deal with a cannabis company, Dixie Brands. If approved by Dixie’s board, Dixie would manufacture an Arizona line of cannabis products, starting with vape pens and edible gummies and later expanding to beverages. Learn more here: https://www.wsj.com/articles/arizona-iced-tea-maker-turns-to-weed-11565172124

Benjamin Caplan, MDArizona Beverage Co embracing cannabis too
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Video: Controversial Questions in Cannabis Today

As cannabis finds its place back into modern human culture quickly, there is much still to be learned. As the science grows and adapts to modern need and expectations, the “can we” may be out-pacing the “should we.” On the other hand, there are circumstances where modern culture really “should be” and is handicapped by years of misinformed stigma.

Here, a few controversial questions about cannabis:

Should teachers be allowed to use cannabis around children? 

Should spiritual leaders be allowed to use cannabis, as they have for millennia?

Should taxi drivers be allowed to use cannabis on the job?

Should pilots be allowed to use cannabis?

To explore related information, click the keywords below:

Benjamin Caplan, MDVideo: Controversial Questions in Cannabis Today
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Author’s Response to Discrepancies in Medical Cannabis Use

Medical Cannabis Use: The Authors Reply

In yesterday’s blog post, the discrepancies in the number of medical cannabis users were discussed and the suggestion arose that perhaps medical cannabis use may need stricter regulations. The author of the piece that inspired the letter featured in the post responded, highlighting the possibility that recreational cannabis is being used for medical purposes rather than users obtaining cannabis from more nefarious sources. The author points out that renewing medical licenses can be a hassle and in states where recreational cannabis has been legalized patients may just be obtaining their cannabis, used for medical purposes, from recreational dispensaries. Surveys that delve into this issue are needed to confirm the author’s hypothesis. 

Describing the medical process of obtaining a cannabis license as a hassle is, unfortunately, reported by many consumers. State governments are forced to run the regulatory processes, in the absence of federal support, and conservative politicians and opposition groups often create difficulty around opening dispensaries in their districts. On top of the expenses of renewing or obtaining a medical license, it may seem almost less confrontational for people who reside in a state or have access to recreational marijuana (from a state-regulated dispensary) simply to purchase recreational cannabis, rather than take the time to obtain a license. 

Of note, Massachusetts is one of the few states that has anticipated this circumstance and has codified protections and advantages of the medical program, into law. In Massachusetts, medical patients are incentivized through robust discounts (totaling greater than $2000 in discounts, and 20% cost reduction because of the absence of state taxation for medical patients.) Further, there are legal protections available only to medical patients, and the opportunity for delivery, which are not available to recreational consumers.

Benjamin Caplan, MDAuthor’s Response to Discrepancies in Medical Cannabis Use
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The Effect of Cannabis Consumption on Sperm

Impacts of cannabinoid epigenetics on human development- reflections on Murphy et. al. ‘cannabinoid exposure and altered DNA methylation in rat and human sperm’ epigenetics

An op-ed has praised the work published last year which exposed how pre-conception exposure to cannabis in males is related to alterations in epigenetic regulation of the central nervous and immune systems. Murphy et. al.’s paper ‘Cannabinoid exposure and altered DNA methylation in rat and human sperm,’ revealed that the sperm cells of men who have consumed cannabis are a key vector that may affect neuraxis, heart blood vessels, immune stimulation, secondary genomic instability, and carcinogenesis in the fetus offspring. The author of the response piece extrapolates the data collected by Murphy et. al. to conclude the genome-epigenome is extremely sensitive to environmental toxicants and that further research should examine the epigenomic toxicology of multiple cannabinoids. 

The effect of prenatal exposure to cannabis on birth rates, birth outcomes, and the health of the mother is still uncertain. Studies focussing on cannabis use during pregnancy are limited, and what little has been reported, is inconsistent. The featured article now brings to light that both parents may need to be cautious when attempting to conceive or when having unprotected sex as cannabis may affect both germ cells. Currently, governing bodies of obstetricians advise that pregnant mothers cease any cannabis use so if someone who needs cannabis for a medical purpose that improves their quality of life becomes pregnant they need to seek out alternative methods of treatment. Research is needed so that pregnant women can safely continue their medication or so that alternatives can be found so that women do not need to suffer for the duration of their pregnancy and possible breastfeeding period. 

View this review (yellow link) or download:

This paper is also stored here:    http://bit.ly/2K42H1S     inside the CED Foundation Archive

To explore related information, click the keywords below:

Benjamin Caplan, MDThe Effect of Cannabis Consumption on Sperm
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Woman-owned Cannabis in MA

Looking to support small businesses? Or women in cannabis? Caroline Frankel, owner of Caroline’s Cannabis, launched her dispensary in Uxbridge, MA earlier this year. Frankel’s boutique cannabis shop opened without the backing of wealthy investors, a board of directors, or an expensive legal team. The company is the first woman-owned small business and the first general applicant to be awarded a final license. Learn more here: https://www.carolinescannabis.com

Benjamin Caplan, MDWoman-owned Cannabis in MA
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Cannabis: Vaporizing vs Smoking

Smoking cannabis brings toxins and unhealthy combustion byproducts into the body. With temps in the ~2000’F range for flame, burning flower incinerates a large portion of the product being consumed. As the distance from the point of flame grows, temperatures are lower, and cannabinoids are vaporizing, in addition to being burned by the flame. Over time, as heating technology has improved, there is no longer a need for blasting temperatures way beyond what the material can safely sustain before turning to tar and ash.

Beyond developed habits of consumption, social familiarity, and simplicity of use, one of the reasons many enjoy combustion is the other effects of heat. As with any human contact with extreme heat, blood rushes to the source of heat, and this may present a platform, through which cannabinoids may enter the bloodstream more quickly. The extravagant heat is also aerosolizing many more cannabis compounds than vaporization temperatures typically support, so the effect of flame is often felt to be more intense.

Vaporizing cannabis, however, is less likely to introduce mutations in the polyphenol compounds found in abundance within cannabis, and some of the mutations create terrible molecules known to be caustic and destructive.

If the medical rationale for vaporizing (over combustion) is not convincing, please consider the financial argument: Though purchasing a vaporizer may be costly, it’s a smart investment that could save money in the long run. Learn more by watching this video:

Benjamin Caplan, MDCannabis: Vaporizing vs Smoking
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