Fatty Acid Amide Hydrolase and Monoacylglycerol Lipase Inhibitors Produce Anti-Allodynic Effects in Mice Through Distinct Cannabinoid Receptor Mechanisms
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Unlabelled The endocannabinoids anandamide and 2-arachidonoylglycerol are predominantly regulated by the respective catabolic enzymes fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL). Inhibition of these enzymes elevates endocannabinoid levels and attenuates neuropathic pain. In the present study, CB₁ and CB₂ receptor-deficient mice were subjected to chronic constriction injury (CCI) of the sciatic nerve to examine the relative contribution of each receptor for the anti-allodynic effects of the FAAH inhibitor, PF-3845, and the MAGL inhibitor, JZL184. CCI caused marked hypersensitivity to mechanical and cold stimuli, which was not altered by deletion of either the CB₁ or CB₂ receptor, but was attenuated by gabapentin, as well as by each enzyme inhibitor. Whereas PF-3845 lacked anti-allodynic efficacy in both knockout lines, JZL184 did not produce anti-allodynic effects in CB₁ (-/-) mice, but retained its anti-allodynic effects in CB₂ (-/-) mice. These data indicate that FAAH and MAGL inhibitors reduce nerve injury-related hyperalgesic states through distinct cannabinoid receptor mechanisms of action. In conclusion, although endogenous cannabinoids do not appear to play a tonic role in long-term expression of neuropathic pain states, both FAAH and MAGL represent potential therapeutic targets for the development of pharmacological agents to treat chronic pain resulting from nerve injury.Perspective This article presents data addressing the cannabinoid receptor mechanisms underlying the anti-allodynic actions of endocannabinoid catabolic enzyme inhibitors in the mouse sciatic nerve ligation model. Fatty acid amide hydrolase and monoacylglycerol lipase inhibitors reduced allodynia through distinct cannabinoid receptor mechanisms. These enzymes offer potential targets to treat neuropathic pain.
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Other studies using knockout mice or selective inhibitors of CB1 or CB2 receptors show no alterations of nociceptive behavior in neuropathic pain models.
“However, other studies using knockout mice or selective inhibitors of CB 1 or CB 2 receptors show no alterations of nociceptive behavior in neuropathic pain models (Kinsey et al, 2009(Kinsey et al, , 2010) ) though ceiling effects and other methodological differences between studies may have precluded the detection of enhanced nociceptive behavior.”
From The endogenous cannabinoid system: a budding source of targets for treating inflammatory and neuropathic pain (2018) · cites this paper as Kinsey et al, 2010
Ceiling effects and other methodological differences between studies may have precluded the detection of enhanced nociceptive behavior in neuropathic pain models.
“though ceiling effects and other methodological differences between studies may have precluded the detection of enhanced nociceptive behavior.”
From The endogenous cannabinoid system: a budding source of targets for treating inflammatory and neuropathic pain (2018) · cites this paper as Kinsey et al, 2010
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- Authors
- Kinsey, S. G., Long, J. Z., Cravatt, B. F., & Lichtman, A. H.
- Affiliations
- Virginia Commonwealth University (US)
- Scripps Research Institute (US)
- Corresponding author
- Kinsey, Steven G.
- Venue
- The Journal of Pain
- Publisher
- Elsevier BV
- Published
- 2010-12
- Volume
- 11
- Issue
- 12
- Pages
- 1420-1428
- ISSN
- 1526-5900 (ISSN-L)
- PMC
- PMC2962430
- OpenAlex
- W2084283702
- Cited by
- 118
- References
- 42
- Citations by year
- 2026: 2 · 2025: 1 · 2024: 5 · 2023: 2 · 2022: 3 · 2021: 6 · 2020: 4 · 2019: 5 · 2018: 12 · 2017: 6 · 2016: 9 · 2015: 9 · 2014: 17 · 2013: 16 · 2012: 8
- FWCI
- 8.92
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Licence
- Locations
- Journal of Pain (publishedVersion)
- PubMed (publishedVersion)
- PubMed Central (acceptedVersion)
- Funders
- National Heart, Lung, and Blood Institute (R01HL087282)
- National Institute on Drug Abuse (P01DA009789, R01DA015197, P01DA017259, P50DA005274, T32DA007027)
- Topics
- Health Sciences › Medicine › Pharmacology › Cannabis and Cannabinoid Research
- Health Sciences › Medicine › Physiology › Pain Mechanisms and Treatments
- Life Sciences › Neuroscience › Sensory Systems › Ion Channels and Receptors
- Keywords
- fatty acid amide hydrolase, monoacylglycerol lipase, FAAH inhibitors, MAGL inhibitors, endocannabinoids, anandamide, 2-arachidonoylglycerol, CB1 receptor, CB2 receptor, neuropathic pain, allodynia, chronic constriction injury, sciatic nerve, gabapentin, cold allodynia, mechanical allodynia, chronic pain
- MeSH terms
- Fatty Acid Amide Hydrolases, Amidohydrolases, Animals, Enzyme Inhibitors, Female, Male, Monoacylglycerol Lipases, Neuralgia, Sciatic Nerve, Mice, Knockout, Receptor, Cannabinoid, CB1, Receptor, Cannabinoid, CB2, Mice
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