CBD, short for Cannabidiol, has gained widespread popularity as a natural sleep aid. It is often promoted as a way to reduce stress, improve relaxation, and support better rest. But how does CBD actually work in the body? What system does it tap into? What are the exact mechanisms? And is it safe?

In this first part of the article. we’ll explore the Endocannabinoid System and what effect CBD has on it. In the second part we'll focus on it's impact on sleep, potential benefits and concerns.

The Endocannabinoid System

The primary interaction for CBD in the body is through the Endocannabinoid System (ECS). The ECS plays an important role in regulating sleep, mood, stress, pain, and immune functions.

The system loosely consists of the following components:

Endocannabinoids (ECBs)

These are natural cannabinoid compounds that are produced by the body and include:

• Anandamide (AEA), which is associated with relaxation, mood balance, and stress reduction, and
• 2-Arachidonoylglycerol (2-AG), which helps regulating inflammation, immune function, and sleep cycles.

Cannabinoid Receptors

The receptors to which the ECBs bind to and signal their presence in the body. There are two types of receptors:

• CB1 (mainly in the brain & nervous system), which is involved in mood, sleep-wake regulation, memory, and
• CB2 (mostly associated with the immune system), which is involved in inflammation and pain perception.

Enzymes

The molecules that break down ECBs, including:

• FAAH (Fatty Acid Amide Hydrolase), which breaks down AEA, and
• MAGL (Monoacylglycerol Lipase), which breaks down 2-AG.

The ECS is always active and helps maintain homeostasis - the body’s natural balance. When something disrupts this balance (such as stress, injury, illness), the ECS produces endocannabinoids to restore stability.

For instance if you’re sleep deprived, the ECS increases the AEA endocannabinoid, which binds to CB1 receptors in the brain. This reduces stress signalling and helps you unwind. Once relaxation sets in, the FAAH enzyme is released which breaks down AEA and brings it back to baseline.

How CBD interacts with the ECS

Unlike THC, CBD does not directly bind to CB1 or CB2 receptors. Instead, it modulates the ECS indirectly in several ways:

CBD Inhibits FAAH which leads to higher levels of AEA.

By inhibiting the enzyme that breaks down AEA, more AEA remains in the system which increases relaxation levels. AEA is sometimes called the “bliss molecule” due to its calming and mood-enhancing effects.

CBD modulates CB1 receptors to prevent their overstimulation.

CBD acts as a negative allosteric modulator of CB1, meaning it reduces excessive CB1 activation. This prevents overstimulation of CB1 receptors, reducing anxiety without causing the psychoactive effects of THC.

CBD indirectly activates CB2 which reduces inflammation.

By enhancing 2-AG signaling, CBD can indirectly activate CB2 receptors, which regulate inflammation and the immune response. This can reduce pain and inflammation-related sleep disturbances.

CBD influences other receptor systems beyond the ECS.

Serotonin (5-HT1A) Receptors: Improves mood, reduces stress.

GABA Receptors: Promotes relaxation and helps regulate sleep cycles.

TRPV1 Receptors: Reduces pain perception, which can improve sleep in those with chronic pain conditions.

See here for part two of CBD & Sleep where we'll focus on CBD's impact on sleep, potential benefits and the concerns.

Consider consulting with a healthcare professional if you are unsure about a new supplementation regimen to ensure that it’s safe and appropriate for your individual needs.