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Peppered Cannabinoids: Caryophyllene

12/30/2017

Pass the pepper please!

You might have experienced something like this: you eat a pepper and it makes you sweat.

If you haven’t had that experience, try a habanero pepper (just a little) to play along.

Sweating is dependent on our cannabinoid system (CS): for example, CB2 skin receptors modulate/maintain mammalian body temperature.

And it’s not just a reaction to the pepper: the pepper is modulating cannabinoid receptors – especially forehead ones for habanero-eaters – and it seems the hotter the pepper equals more CB2 response.

This happens because of the ubiquitous essential oil caryophyllene.

Here’s a sales site with caryophyllene and black pepper oil information.

And here’s a 2008 NIH article, Beta-caryophyllene is a dietary cannabinoid, which confirms the caryophyllene found in black pepper is “dietary” and states the oil is also found in such things as oregano, cinnamon and cannabis.

Of course, a re-examination of the world spice trade is needed: looks like early cannabinoid trafficking now – who knew?

*Next Up: NYE 2017 and an abstract serotonin poem, A Microbiota Ode to the Brain-Gut Axis.

Posted by Bryan W. Brickner

Toast Them Hemp Seeds For Hempoween

10/31/2017

Toasted Hemp Seeds for Hempoween

Two hundred and fifty-two years ago today, on 31 October 1765, George Hempington celebrated the first documented Hempoween. The farmer and his slaves had harvested 152 bushel of hemp seed; after milling the seed to collect the oil, George writes of his celebratory actions in his farm journal:

“31 October: Finished sowing Wheat in Hemp Ground at Rivr. Plantn. & plowed in a good deal of shattered Hemp Seed – 27 Bushls. in all 152.”

That, my friends, is a traditional Hempoween celebration: the scattering of shattered hemp seeds on your field (or garden) as a fertilizer for the next season.

There are also many more modern ways to enjoy your hemp products this Hempoween: one that was new to me is toasted hemp seeds. I purchased the little delicacies (see picture above) at a regular grocery store in the Midwest – nothing fancy, and no special license or doctor’s note was needed.

I did leave the original bag of toasted seeds with some hippies (burners really), and I don’t expect to see the treats again; you see, they are quite yummy toasted and I know what to expect when one leaves a bag of hemp products around burners.

So toast them hemp seeds this year while you are celebrating Hempoween, and perhaps even give a shout out of remembrance to George, his wife Artha, and the slaves who made it all possible.

Here’s to a happy – and toasted – Hempoween for all!

*Next Up: Sunday 5 November and a pamphlet release, Three Liminal Dialogues on Serotonin, Mosby and Luther.

Posted by Bryan W. Brickner

Homeostasis: If Not Cannabinoid Receptor Three, then Cannabinoid Receptor Third

6/7/2017

The Cannabis Papers by Publius

In The Cannabis Papers: A citizen’s guide to cannabinoids (2011), we noted evidence for a CB3 receptor in addition to CB1 and CB2. The research suggested that there was more happening (things to be accounted for, scientifically) and another receptor was proposed. In 2017 it looks like the best answer is a third category of activity and not a specific receptor; notably, this third activity involves many other kinds of receptors.

The Guide to Pharmacology website has an introduction page for cannabinoid receptors; at the bottom of the page there is a section on this third activity (non-CB1 and non-CB2 modulation). The site notes it is “generally accepted” that other receptor types, and thus other systems, are modulated by cannabinoids; this is true for endo, plant and pharmaceutical cannabinoids.

This third signaling effect connects progesterone and nuclear receptors to cannabinoids; it also suggests modulating endometriosis is similar to homeostasis: both depend on cannabinoids for healing and health.

*Next Up: Wednesday 21 June and a 2020: Virtual Representation and We the People.

Posted by Bryan W. Brickner

Homeostasis: Cannabinoid, Progesterone and Nuclear Receptors

5/31/2017

Nuclear Receptor In Action

Think of a cell as a hub: a center of communication.

This hub has gates and points of entry: for our example, think of cannabinoid and progesterone receptors. These receptors facilitate communication with other hubs and inside a hub (with other cells and inside a cell).

There are nuclear receptors in all hubs/cells; these receptors regulate our genes (by transcribing DNA) and control our development, homeostasis and metabolism.

Recall that endometriosis is a disruption of a hub and its network: the cells grow (generate) as they are designed to do, just in the wrong spot.

An obvious point of disruption and research is the communication between progesterone and nuclear receptors; another is anandamide and all the other cannabinoids (endo, plant and pharmaceutical), as they too can modulate nuclear receptors.

We’ll begin with that homeostatic science next week: cannabinoids modulating nuclear receptors - and thus our every day.

*Next Up: Wednesday 7 June and a Homeostasis: If Not CB Three, then CB Third.

Posted by Bryan W. Brickner

Homeostasis: Endometriosis, Progesterone and Cannabinoid Systems

5/24/2017

Progesterone

Progesterone-dependent regulation of endometrial cannabinoid receptor type 1 (CB1-R) expression is disrupted in women with endometriosis and in isolated stromal cells exposed to 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD)

The above title was published in Fertility and Sterility in 2012 and can be found on PubMed.

The research finds that endometriosis, where cells grow outside instead of inside the uterus (endometrium), is caused by a failure to communicate between progesterone and the cannabinoid system; this failure is painful and contributes to infertility. Summary quote from the research: “Our studies reveal a role for the anti-inflammatory actions of progesterone in regulating endometrial cannabinoid signaling, which is disrupted in women with endometriosis.”

How does that work though? What is disrupted? If communication between progesterone and the CB1 receptor is disrupted (as cells grow, just in the wrong place), how do cells normally communicate in a healthy, undisrupted homeostatic way?

The answer involves cannabinoid and progesterone nuclear receptor signaling: let’s just begin there next week.

*Next Up: 31 May and a homeostatic view of Progesterone Nuclear Receptors and Cannabinoid Systems.

Posted by Bryan W. Brickner

Mental Pictures: Spring and Summer 2017

4/4/2017

Mental Pictures 2017

Here is a blogging mental picture for spring and summer 2017. Three pamphlets: electricity and serotonin, another on Mosby’s Gettysburg, and then one on Martin Luther and popes. We’ll revisit PubMed for cannabinoid and serotonin news and continue with our 2020 visualizations … and more footnotes from Hannah Arendt’s The Human Condition.

Thanks all and ever higher!

Next Up: Sunday 9 April, Usurpation Day 2017, and an Arendt Footnotes on Beginnings.

Posted by Bryan W. Brickner

2020: Yale University, Chicago Tribune and the Sowers of Constitutional Sepsis

9/23/2016

US Constitution Article I

Sepsis is a life-threatening condition that kills more often than heart attacks. It occurs when our bodies begin to injure themselves while trying to fix themselves: symptoms include fever, increased breathing and heart rates, as well as confusion.

I was looking at sepsis for cannabinoid system science and will continue to do so; I also noticed sepsis appears to describe our current polity, a “constitutional sepsis” so to speak.

Then I thought of the sowers of constitutional sepsis, people who know there is an antidote. Sowers of constitutional sepsis discussed on this blog include Yale’s professor of law Akhil Reed Amar and the Chicago Tribune’s Bruce Dold, John Kass and Eric Zorn.

Yale University vs. the Chicago Tribune seems like a fair match-up, particularly since Yale’s Amar is … bluffing.

*Next Up: A 2020 on Saturday 1 October: Clinton, Trump and the Constitutional Enumeration (Census).

Posted by Bryan W. Brickner

2020: Smells Like Umami – Cannabinoid Heteronomy Hubbub

8/20/2016

Tomatoes are rich in umami components

Umami Hets

Umami is one of five basic tastes along with sweetness, sourness, bitterness and saltiness. We can taste umami because of heteronomy (Hets): specifically, the combination of two receptors to form one action. Today’s heteronomy update explained the umami Hets like this:

"Taste T1 receptors are obligate Hets: ‘T1R3 acts as an obligate partner in T1R1/T1R3 and T1R2/T1R3 heterodimers, which sense umami or sweet, respectively.’"

Pharmaceutical cannabinoid research has regressed on the subject of Hets; they see evidence of cannabinoid Hets yet can’t synthetically reproduce them. The update warns: “in a sense, the field is going backward instead of forward.”

Basic Pharmacological and Structural Evidence for Class A G-Protein-Coupled Receptor Heteromerization
Frontiers in Pharmacology ~ 31 March 2016
Abstract
Cell membrane receptors rarely work on isolation, often they form oligomeric complexes with other receptor molecules and they may directly interact with different proteins of the signal transduction machinery. For a variety of reasons, rhodopsin-like class A G-protein-coupled receptors (GPCRs) [Cannabinoids] seem an exception to the general rule of receptor–receptor direct interaction. In fact, controversy surrounds their potential to form homo- hetero-dimers/oligomers with other class A GPCRs; in a sense, the field is going backward instead of forward. This review focuses on the convergent, complementary and telling evidence showing that homo- and heteromers of class A GPCRs exist in transfected cells and, more importantly, in natural sources. It is time to decide between questioning the occurrence of heteromers or, alternatively, facing the vast scientific and technical challenges that class A receptor-dimer/oligomer existence pose to Pharmacology and to Drug Discovery.

*Next Up: The Union 2016 summer series continues on Saturday 27 August with part 9, Johnny Reb and Gus Kotka Nowhere Nobody Home.

Posted by Bryan W. Brickner

2020: Bivalent Ligands Targeting Cannabinoid Receptors? Longer Linkers May Not Be The Solution

7/9/2016

CNR1 is CB1 genetics

CB1 pharmacophore

Today’s cannabinoid system science update looks at a piece of pharmaceutical research on bivalency and our CB1 receptors. Pharmaceutical researchers are trying to duplicate the cannabinoid bivalency trait found in our bodies, which is the ability to simultaneously influence two different kinds of receptors.

They understand what our bodies do (“evidence suggests that ligands enter CB1 through the lipid bilayer”) yet don’t know how to copy it (“linkers are unlikely to exit the receptor through its external face”). They conclude: “the entire premise of designing bivalent ligands targeting CB1 must be revisited.”

Our bodies keep doing the bivalency shuffle, all the time and every day, while the pharmaceutical researchers revisit the drawing board, and maybe (perhaps) take Nixon’s scheduling law with them.

Trends in Pharmacological Sciences
PubMed 2016
One for the Price of Two…Are Bivalent Ligands Targeting Cannabinoid Receptor Dimers Capable of Simultaneously Binding to both Receptors?

Abstract:
Bivalent ligands bridging two G-protein-coupled receptors (GPCRs) provide valuable pharmacological tools to target oligomers. The success of therapeutically targeting the cannabinoid CB1 receptor has been limited, in part due to its widespread neuronal distribution. Therefore, CB1 ligands targeting oligomers that exhibit restricted distribution or altered pharmacology are highly desirable, and several bivalent ligands containing a CB1 pharmacophore have been reported. Bivalent ligand action presumes that the ligand simultaneously binds to both receptors within the dimeric complex. However, based on the current understanding of CB1 ligand binding, existing bivalent ligands are too short to bind both receptors simultaneously. However, ligands with longer linkers may not be the solution, because evidence suggests that ligands enter CB1 through the lipid bilayer and, thus, linkers are unlikely to exit the receptor through its external face. Thus, the entire premise of designing bivalent ligands targeting CB1 must be revisited.

Next Up: The Union 2016 summer series continues on Sunday 10 July with part 4, Johnny Reb and Gus Kotka Nowhere Enemy Is Time.

Posted by Bryan W. Brickner

2020: Putamen Cannabinoids and Opioids Control Our Brains (Even the brains of presidential candidates)

6/12/2016

Purple is Caudate Nucleus and Putamen / Orange is Thalamus

Brains presidential

There are cannabinoid (pot) receptors and precursors all over our brains; there are also opioid (heroin, morphine, oxycodone) receptors and precursors there too.

“If you were” to click on the publication image below you’d find a schematic representation of our brain’s cannabinoid and opioid receptors. The “If you were” is because there is some caution involved; seems that after looking at the image for a bit (twenty seconds or so) one might see the image looking back at you: I’m just saying it might happen.

I looked at the image for a bit and can report it shows three levels of receptor density for both cannabinoids and opioids: low, moderate and high. Some parts of our brains are high in both; one such spot is the caudate putamen.

The caudate putamen, located at the center of our brains (and the brains of all presidential candidates, it should be said), is fundamental to movement and learning; basically, we wouldn’t be bipedal or remember much without it. Adding science to our sense of ourselves, and the discussion known as the 2016 presidential election, will help us get through the next big thing: the 2020 Enumeration, i.e., the census and the “thirty Thousand.”

Interactions of the opioid and cannabinoid systems in reward: Insights from knockout studies
Frontiers in Pharmacology
Pubmed: 5 FEB 2015

From the abstract: The opioid system consists of three receptors, mu, delta, and kappa, which are activated by endogenous opioid peptides (enkephalins, endorphins, and dynorphins). The endogenous cannabinoid system comprises lipid neuromodulators (endocannabinoids), enzymes for their synthesis and their degradation and two well-characterized receptors, cannabinoid receptors CB1 and CB2. These systems play a major role in the control of pain as well as in mood regulation, reward processing and the development of addiction. Both opioid and cannabinoid receptors are coupled to G proteins and are expressed throughout the brain reinforcement circuitry.

*Images from this publication
See all images (1)Free text

Next Up: Announcing the release of an Ew Publishing research pamphlet, Aspasia of Miletus: Socrates’ Didaskalos, on Wednesday 15 June.

Posted by Bryan W. Brickner