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GPR119: An Exciting Potential Cannabinoid Receptor For Diabetics

Posted by administrator on 3/8/2017
Before we talk about GPR119 and it's potential benefit for diabetics, we need to provide you with some context so you can appreciate how incredibly exciting this news truly is! We also want you to understand better how we know about it -- that we're not just throwing out wild guesses!

We spend a lot of time reading consumer oriented information sources for the latest news and scientific information on cannabis research. We're talking about resources like Project CBD, High Times, Leafly, Medical Jane, and Leaf Science. While we applaud these sources for getting the word out about the benefits of CBD oil, we've found that they often miss some of the most important news coming out in the scientific literature about cannabinoids, the endocannabinoid system, and how full spectrum CBD oil may prove to be the natural version of several prescription drugs that are currently in development.

One important topic where there is scant information in these consumer oriented information sources is the whole topic of "novel cannabinoid receptors," also sometimes called "orphan cannabinoid receptors." These are known cell membrane receptors that researchers strongly suspect may actually be part of the endocannabinoid system, just like CB1 and CB2. These suspicions are based on solid science: the specific molecules they respond to, their gene sequences, their functionality, their physical shape, and how they interact with the entire endocannabinoid system. It also looks like at least some of these receptors will be officially named cannabinoid receptors (like CB3, CB4, and so on) in the near future as scientists gather an increasing amount of evidence that they are indeed part of the endocannabinoid system, just like CB1 and CB2.

GPR119 is one of the most likely candidates to be named a new cannabinoid receptor. GPR119 is a cell membrane receptor that responds in specific ways to specific chemical molecules in an almost "lock and key" fashion. GPR119 receptors are found primarily on the cell membranes of beta cells in the pancreas and on enteroendocrine L cells of the third and last segment of the small intestine (the ileum), the large intestine, and the pancreas. 

Beta cells are responsible for secreting insulin and enteroendocrine L cells are responsible for secreting incretins. Insulin is one of the most powerful hormones known and affects the human body in a variety of different ways. It's most famous role is in transporting glucose (blood sugar) across the cell membrane to the inside of cells all over the body so they can use glucose for energy. Incretins are a class of hormones. While they're not as much of a household name as insulin, they are just as powerful and really should be as famous as insulin. They have the ability to slow what is known as "gastric emptying" which is the process by which the stomach moves food it receives out and into the rest of the gastrointestinal system, and thereby, how fast glucose is released into the body after a meal. Incretins can also lower blood glucose levels by slowing the release of another hormone called glucagon, which is released from alpha cells in the pancreas and raises the level of glucose after a meal.... glucagon is basically the opposite from insulin in its function.

Even if you don't quite understand the long paragraph above, pay close attention to the bottom line of what this all means:
- The hormonal mechanisms described above are CRITICAL to preventing, controlling, and possibly even curing diabetes!!! 
- The action of these hormones are also critical to regulating metabolism and preventing obesity!
- The GPR119 receptor is located on the cell membranes of the exact cells where these powerful hormones are produced!
- The scientific research so far shows that stimulating the GPR119 receptor regulates the action of these hormones and related physiological processes!

So, how do we know all this if it isn't being talked about in the consumer oriented news sources for cannabis research?

We read actually read highly technical scientific journals...
It's amazing what you can dig up if you're willing to spend hours poking around in rather obscure scientific literature that isn't even available online. Well, only the abstracts are available online for free. Take this for example. After scouring through a twenty-one page, highly technical report published in October 2009 in the obscure journal, "Expert Opinion on Therapeutic Patents," one thing became abundantly clear:
Synthetic chemicals, basically synthetic cannabinoids, that specifically and strongly target the receptor, GPR119, are going to be the next generation of type 2 diabetes medications to flood the market in the not so distant future.
This very revealing paper was written by industry insiders, who also happen to be astute scientists from the pharmaceutical company, Arena Pharmaceuticals, based in San Diego.

A good percentage of this paper was devoted to covering all the patents that different pharmaceutical companies had been filed for -- and it was patent application galore -- so much so it almost boggles the mind!!! Obviously, the race was on to engineer synthetic chemicals in the lab (agonists) to stimulate the GPR119 cell membrane receptor and then patent those so they could be developed into a prescription drug to sell at hefty profits to the enormous number of people who now have diabetes or who are likely to develop diabetes in the near future (they went through those alarming stats too).

Besides describing the science in highly accurate detail, the authors of this paper went through the patent applications for ten pharmaceutical companies: Yamanouchi Pharmaceutical Co., Astellas (Yamanouchi Pharmaceuticals is now a part of Astellas), Arena Pharmaceuticals, Prosidion Ltd, GlaxoSmithKline (was Smith-Kline Beecham), Merck, Biovitrum, Novartis/IRM, Schering Corp, Bristol-Myers Squibb. All of these companies had applied for MULTIPLE patents on the synthetics they were creating to target GPR119. Plus, there was a note at the end of the paper that more pharmaceutical companies had filed for patents on synthetic chemicals that could trigger the GPR119 receptor since they had completed the paper..... and that was in 2009... there are way more patents filed on this since!!!


When pharmaceutical companies develop these types of very specific synthetic chemicals to very specifically target a cannabinoid receptor (and other cell membrane receptors), they usually model this on naturally produced endogenous (produced inside the body) cannabinoids AND on plant (mostly cannabis) cannabinoids that are already known to interact specifically with those receptors. Yes, they tweak the chemical structure, supposedly to "improve" their function, but the main reason they tweak them is that they cannot patent a natural chemical produced by the human body or a natural chemical extracted out of the oil of the cannabis plant. For them to patent it, and turn it into a drug that they can sell at a hefty profit, it must be something they develop themselves. It must be something that is unique enough in some way that the patent office will issue them a patent. Otherwise, it would not be profitable to them.

Think about that a while! Let it sink in!

Now, we cannot yet find specific information on whether or not CBD or any of the other cannabinoids found in CBD oil is capable of directly stimulating or blocking, i.e targeting, the GPR119 cell membrane receptor. However, we do know that CBD has been shown in well designed scientific studies to lower the blood sugar of diabetic rats very significantly. We also know that CBD is known to stimulate the production of oleoylethanolamide (OEA), a chemical that is now known to directly stimulate the GPR119 receptor! OEA is considered a cannabinoid by some scientists and a "cannabinoid-like" chemical (a agonist ligand of cannabinoid receptors for any science nerds out there) or a "pseudo-cannabinoid" by other scientists. So, CBD at minimum indirectly affects the GPR119 cell membrane receptor!

By the way, if a targeting chemical to a cell membrane receptor acts like a cannabinoid, and quacks like a cannabinoid, shouldn't it be called a cannabinoid? Functionally, it definitely is a cannabinoid! Some scientists are just having a hard time wrapping their heads around the idea that cannabinoids should be more broadly defined than originally thought when the cannabinoids to CB1 and CB2 were discovered and studied. That's why the terminology is in flux and somewhat debated, although the underlying mechanisms have become quite clear in some cases.

At any rate, it can be stated that CBD oil very likely provides the cannabinoids that can stimulate the GPR119 receptor, directly and or indirectly, in ways that can help diabetics and those struggling with obesity and metabolic disorders. Stay tuned for more very exciting news on this front and remember you heard it here first!

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