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I recently got asked a question about sleep and sleep regulation. This works under the endocannabinoid system (ECS) and is an excellent example of how your body regulates a primary function we all experience. It also presents an opportunity to discuss how we might view medicine and conditions like sleep deprivation with new eyes. So how is sleep regulated? At a lesser level by something called adenosine. This is actually what caffeine from coffee affects and why it can give us a “pick me up.” At a higher level, you have an endocannabinoid neurotransmitter called oleamide. Oleamide (which we’ll cover later in this article) is not discussed nearly as much as its cousins, anandamide, and 2-AG, the principal ECS neurons.

Related: Terpenes and Cannabinoids

An Introduction to the Endocannabinoid System

The endocannabinoid system enables signaling between different cells to regulate various activities in the body. The ECS is made up of several parts:

If those enzymes break down cannabinoids once they’ve done their job, what is that job? That’s a great question! And it’s one that many scientists are still working to answer years after discovering this biological system.

Here’s what we know:

At a fundamental level, the endocannabinoid system helps maintain homeostasis throughout the body. Homeostasis refers to the biological stability and balance needed to maintain our health and overall well-being. The ECS plays a crucial role in maintaining this balance and physiological function.

What the Endocannabinoid System Regulates: Sleep and More

To deliver this homeostatic balance, the endocannabinoid system regulates various physiological processes, including:

We’ve identified six different endogenous cannabinoids that our bodies produce, with the two most well-known and well-studied being ANA and 2-AG.

We also know of two cannabinoid receptors (CB1 and CB2) located in cells throughout our body. We have CB1 receptors in our brain, central nervous system, organs, blood vessels, skin, and intestinal tract. Most CB2 receptors are found in the cells of our immune system.

Cannabinoids, Sleep, and More: How the ECS Works

Endogenous cannabinoids bind with those two receptors and trigger signals in the body to produce a physiological response. That response can launch various processes, like an immune response to pain, produce more or less mood-regulating hormones, and stimulate relaxation, drowsiness, or wakefulness. But it can do so much more.

Depending on which cells are being acted upon by the receptors and which cannabinoids are unlocking them, a wide range of biological activities can happen. For example, when CB1 receptors activate in the brain, it can affect how our body stores energy and metabolizes it.

Cannabinoids from sources found outside the body (exogenous cannabinoids) also interact with our endocannabinoid system. If you stop to think about it, it’s amazing that the ECS went undiscovered for so long when it plays such a significant role in our bodies. It wasn’t discovered until the early 90s when scientists were investigating the effects of the best-studied cannabinoid found in the cannabis plant: THC.

Before this discovery, we had no idea that the human body produced its own cannabinoids or had an internal system to interact with exogenous cannabinoids. Since discovering the endocannabinoid system, researchers have determined that it’s ancient in evolutionary terms —  they traced it back to living organisms from over 500 million years ago.

Cannabinoids for Sleep: The Endocannabinoid System’s Role

A woman sleeping under the covers

Our sleep-wake cycles show homeostasis in action — they are an ongoing, dynamic balance of rest and activity that’s essential for our vitality, health, and survival. Our homeostatic sleep drive works with circadian processes to transition us between wakefulness and sleep throughout the day. And the endocannabinoid system influences our sleep in various ways.

Related: CBDa, CBGa, and THCa

Cannabis and Its Interaction With the ECS

Cannabis contains many naturally-occurring cannabinoids, with the most well-known and studied being THC and CBD. These cannabinoids signal processes in the endocannabinoid system to do various things, from relieving pain and changing aspects of cognition to promoting wakefulness or sleep to ease insomnia.

For example, THC is a cannabinoid that binds to both receptors, which is why it can have such a profound effect on the body. On the other hand, CBD acts quite differently and doesn’t bind to the CB1 or CB2 receptors. However, it might bind to an endocannabinoid receptor that we haven’t discovered yet. From what we know so far, CBD appears to change how those two receptors interact with the endogenous cannabinoids that our body naturally produces.

Oleamide: A Lesser-Known Cannabinoid for Sleep

Oleamide builds in our spinal column the longer we are awake. As oleamide builds, it influences other neuro systems, which cause “sleepiness” and a “downregulation” of our bodies. For example, the GABA neuro-system is affected by oleamide. Oleamide causes an upregulation in our GABA channel, which results in a decreased “energy” state. By understanding this “point of regulation,” we can now influence this process. The cool thing is that, generally, you control the way your body wants to go with natural products, which is a healthier/better/more efficient regulation. We could “improve” this point of regulation by presenting oleamide pre-cursors (effectively increasing the resource your body is trying to work with) or by playing with how quickly your body will dissipate or hydrolyze oleamide (increasing or decreasing concentrations).

Our bodies are extraordinary mechanisms that operate pretty simply at the top level. By understanding how our bodies work (endocannabinoid system/hypothalamus/hippocampus) and what resources our bodies use to do this work (many things in nature in our food supply), we can literally “engineer” very safe effectors that work!

A colorful abstract drawing of the brain

Related: B-caryophyllene & the ECS

There’s so much more to learn here — the endocannabinoid system’s existence reveals a fascinating connection between various cannabinoids and a crucial component of our body’s health: sleep-promoting biology. It’s no wonder that the cannabis plant continues pushing forward the forefront of therapeutic research for health disorders, pain, mood, and sleep.

Looking for solutions to your poor sleep? Learn about our GnuPharma Care Plan and how we can help identify imbalances in the endocannabinoid system to help you get your sleep back on track.