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Study breakdown

Mice Without the Anandamide Breakdown Enzyme Were More Sensitive to THC-Like Effects of Other Cannabinoids

Animal StudyPreliminary evidence
The takeaway

Mice genetically lacking the enzyme FAAH, which breaks down the endocannabinoid anandamide, showed enhanced sensitivity to the subjective-like effects of anandamide and a MAGL inhibitor in a THC discrimination task.

Readers interested in the neuroscience of how natural cannabinoids and THC produce their effects.

Anandamide fully mimicked THC only when its breakdown enzyme was absent

What the researchers found

Researchers compared mice lacking fatty acid amide hydrolase (FAAH), the enzyme primarily responsible for breaking down anandamide, with normal mice in a drug discrimination test using THC.

Both groups learned to discriminate THC at similar rates and showed similar THC dose-response curves. However, anandamide fully substituted for THC only in FAAH knockout mice, not in normal mice. A metabolically stable anandamide analog worked in both groups but was more potent in knockouts.

The MAGL inhibitor JZL184, which boosts 2-AG levels, produced near-full THC-like effects in normal mice and full substitution in FAAH knockouts. Combined FAAH and MAGL inhibition produced similar effects in both groups.

Why it matters

Understanding how the endocannabinoid system's own signaling molecules produce THC-like effects informs research on both cannabis pharmacology and potential therapeutic approaches that target endocannabinoid metabolism rather than directly activating cannabinoid receptors.

The numbers in context

THC training dose: 5.6 mg/kg. Anandamide fully substituted for THC in FAAH knockouts but not wildtypes. JZL184 produced near-full substitution in wildtypes and full substitution in knockouts. Brain anandamide was elevated in FAAH knockouts. JZL184 increased 2-AG levels equally in both genotypes.

How the study worked

FAAH knockout and wildtype mice were trained to discriminate THC (5.6 mg/kg) from vehicle in a two-lever operant task. Various cannabinoid compounds were tested for substitution. Brain endocannabinoid levels were quantified. The CB1 antagonist rimonabant was used to confirm receptor involvement.

What this study cannot tell us

Drug discrimination in mice does not directly translate to human subjective experiences. Genetically engineered mice may have developmental compensations that differ from pharmacological enzyme inhibition. The study examined acute effects and may not reflect chronic exposure patterns.

How to read the evidence

This is an animal study using genetically modified mice. It provides mechanistic insights about endocannabinoid pharmacology that require validation in other contexts.

When this study was published

Published in 2015. Research on FAAH inhibitors as potential therapeutics has continued with some clinical trials in humans.

The bigger picture

This study illustrates that THC's subjective effects can be mimicked by boosting the brain's own cannabinoids. The finding that FAAH knockout mice respond normally to THC despite having chronically elevated anandamide suggests that baseline endocannabinoid tone does not alter THC sensitivity, a nuance relevant to developing FAAH inhibitor therapeutics.

Questions still open

  • Would FAAH inhibitors produce THC-like subjective effects in humans? How does chronic elevation of one endocannabinoid affect sensitivity to changes in the other?

Common questions

Does this mean anandamide normally produces a high like THC?
Under normal conditions, anandamide is broken down too quickly by FAAH to accumulate to levels that mimic THC. Only when FAAH is absent or inhibited does anandamide build up enough to produce THC-like effects in this test.
Why would researchers want to boost endocannabinoids instead of just using THC?
Boosting the brain's own cannabinoids at sites where they are naturally released could potentially provide therapeutic benefits with greater specificity and fewer side effects than flooding all cannabinoid receptors with THC.

Read the original research

Phenotypic assessment of THC discriminative stimulus properties in fatty acid amide hydrolase knockout and wildtype mice.

Neuropharmacology, 93, 237-42

Citation

Walentiny, D Matthew; Vann, Robert E; Wiley, Jenny L. (2015). Phenotypic assessment of THC discriminative stimulus properties in fatty acid amide hydrolase knockout and wildtype mice.. Neuropharmacology, 93, 237-42. https://doi.org/10.1016/j.neuropharm.2015.02.004

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