Author: Fred Gardner

Makriyannis Lab Determines Structure of the CB1 Receptor

Crystal Structure of the Human Cannabinoid Receptor CB1  was published in Cell October 20, 2016. Thanks to Dale Deutsch for sending the link. Seems like big news. Don’t know how we missed it. Highlights: •AM6538 is presented as a stabilizing, tight binding antagonist of CB1 •Crystal structure of human CB1 in complex with AM6538 is determined •Molecular docking predicts CB1 binding modes of THC and synthetic cannabinoids •Resolution of the binding pocket provides path for rational CB1 drug design Summary: Cannabinoid receptor 1 (CB1) is the principal target of Δ9-tetrahydrocannabinol (THC), a psychoactive chemical from Cannabis sativa with a wide range of therapeutic applications and a long history of recreational use. CB1 is activated by endocannabinoids and is a promising therapeutic target for pain management, inflammation, obesity, and substance abuse disorders. Here, we present the 2.8 Å crystal structure of human CB1 in complex with AM6538, a stabilizing antagonist, synthesized and characterized for this structural study. The structure of the CB1-AM6538 complex reveals key features of the receptor and critical interactions for antagonist binding. In combination with functional studies and molecular modeling, the structure provides insight into the binding mode of naturally occurring CB1 ligands, such as THC, and synthetic cannabinoids. This enhances our understanding of the molecular basis for the physiological functions of CB1 and provides new opportunities for the design of next-generation CB1-targeting pharmaceuticals.  ...

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Cannabis Clinicians Break Into “The Literature”

The journal Epilepsy & Behavior has just published a special issue entitled “Cannabinoids and Epilepsy” that includes a paper by Drs. Dustin Sulak, Russell Saneto, and Bonni Goldstein, “The current status of artisanal cannabis for the treatment of epilepsy in the United States.”  Here’s the abstract: The widespread patient use of artisanal cannabis preparations has preceded quality validation of cannabis use for epilepsy. Neurologists and cannabinoid specialists are increasingly in a position to monitor and guide the use of herbal cannabis in epilepsy patients. We report the retrospective data on efficacy and adverse effects of artisanal cannabis in Patients...

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Publicizing the NAS Report

“Oh, that this 2/2 too sullied flesh would melt…” —Hamlet A report called The Health Effects of Cannabis and Cannabinoids: The Current State of Evidence and Recommendations for Research, released in January by the National Academies of Sciences, Engineering, and Medicine (NAS), was the subject of a “Stakeholders Engagement Meeting” streamed from the NAS building in Washington, DC yesterday.  It can be viewed here INFO TK in its entirety. Meanwhile, here are some screenshots and editorial comments.  The authors of the report were evaluating what they called the “strength of the ‘evidence'” regarding the health benefits and risks of cannabis as medicine. By far the strongest evidence, from their perspective, are randomized, placebo-controlled clinical trials (RCTs). Clinical evidence —the findings and observations of physicians who monitor cannabis use by patients— is ignored completely. It’s not even “low quality!” Retro Messages: 1. The number-one finding makes cannabis use at a young age seem causal when in fact it is a response to an environment (family, neighborhood, school) from which the young user seeks relief.   2.Women who experience nausea during pregnancy tend to smoke more and eat less. And it may be that the Endocannabinoid System, in its wisdom, is making for a slightly easier delivery. The pot-users’ babies gain weight fast and in about a month have caught up with the abstainers’ babies. 3. Cannabis smoking doesn’t exacerbate COPD, according to the great UCLA pulmonologist Donald...

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‘Stakeholder Engagement Meeting’ on NAS Report

Sorry for the late notice —the discussion starts at 9:45 a.m. Beltway Time. Do the organizers not know that most of the “stakeholders” they intend to “engage” are living on the Left Coast? Oh, well… As Wanda used to say, “Be there or be in DARE!” On February 21, 2017, the National Academies of Sciences, Engineering, and Medicine (the National Academies) will host an open stakeholder engagement meeting in Washington, D.C., to discuss key messages from the new report, The Health Effects of Cannabis and Cannabinoids: The Current State of Evidence and Recommendations for Research.  The event, which will also be...

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It’s News in New York: Cannabis for the Elderly

The New York Times has broken the news that medicinal cannabis can be a boon for nursing home residents. The front-page  piece by Winnie Hu February 20 notes that California is far ahead of New York in making the herb available to the elderly. Hu reports that the Hebrew Home at Riverdale is “taking the unusual step of helping its residents use medical marijuana under a new program to treat various illnesses with an alternative to prescription drugs.” Whereas, “A medical marijuana education and support club started by residents of Rossmoor Walnut Creek, a retirement community east of San...

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Improving Microbial Detection Standards for Cannabis

By Kevin McKernan February 8, followed by an editorial retro message. On February 7, the Daily Mail reported a cancer patient in northern California died from a fungal infection that authorities suspect was caused by the inhalation of contaminated medical cannabis. This tragic result, unfortunately, comes as no surprise to our team at Medicinal Genomics.  Since 2015, Medicinal Genomics has been studying the spectrum of microbes that can be found on medicinal Cannabis.  As a result of this research, our company has published two papers warning the community that the widely-used method for detecting microbial contamination on cannabis, petri dish...

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Is the FDA Worth Defending?

When the crude rightwingers take over, the sophisticated liberals start looking not-so-bad in the rearview mirror. We tend to forget how effectively they served the corporations. As the TrumPence Administration sets about destroying the Food & Drug Administration, I’m thinking twice about publishing in O’Shaughnessy’s a list of  35 FDA-approved pharmaceuticals that had to be withdrawn from the market when they proved harmful. I intended to run it because the FDA promotes the cult of the Randomized Controlled Trial —a cult that upholds marijuana prohibition. The Biomedical Establishment disparages all other formats in which evidence of safety and evidence might be...

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Merckantilism

By Fred Gardner    Merck’s CEO Ray Gilmartin announced a “voluntary recall”  of Vioxx on September 30, 2004. Evidence that using Vioxx doubled a patient’s risk of suffering a heart attack or stroke —based on a review of 1.4 million patients’ records— was about to be published in Lancet by David Graham, MD, an FDA investigator.  The FDA director’s office, devoted valet of Big PhRMA, had contacted the Lancet in a futile effort to stop publication of their own scientist’s findings! The US Food and Drug Administration had initially approved the novel painkiller in May 1999 (after a hasty “priority...

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Merck Pays a Pittance for Mass Deaths

 By Fred Gardner November 29, 2011 One of the most downplayed stories of our time ended with a whimper this week.  “Merck has agreed to pay $950 million and has pleaded guilty to a criminal charge over the marketing and sales of the painkiller Vioxx,” the New York Times reported Nov. 23 (in the business section, where important medical news is usually found).  The pharmaceutical giant copped to a misdemeanor: urging MDs to prescribe Vioxx for Rheumatoid Arthritis prior to 2002, when the Food & Drug Administration approved its use for that disorder. The FDA had initially approved Vioxx (after...

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