Cited by 476Cannabis and Cannabinoid ResearchPain Mechanisms and TreatmentsIon Channels and Receptors

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The Endocannabinoid System and Pain

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Guindon, Josee, Hohmann, Andrea·2009·CNS & Neurological Disorders - Drug Targets

DOI 10.2174/187152709789824660PMC PMC2834283

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Abstract

The therapeutic potential of cannabinoids has been the topic of extensive investigation following the discovery of cannabinoid receptors and their endogenous ligands. Cannabinoid receptors and their endogenous ligands are present at supraspinal, spinal and peripheral levels. Cannabinoids suppress behavioral responses to noxious stimulation and suppress nociceptive processing through activation of cannabinoid CB(1) and CB(2) receptor subtypes. Endocannabinoids, the brain's own cannabis-like substances, share the same molecular target as Delta(9)-tetrahydrocannabinol, the main psychoactive component in cannabis. Endocannabinoids serve as synaptic circuit breakers and regulate multiple physiological and pathological conditions, e.g. regulation of food intake, immunomodulation, inflammation, analgesia, cancer, addictive behavior, epilepsy and others. This review will focus on uncovering the roles of anandamide and 2-arachidonoylglycerol, the two best characterized endocannabinoids identified to date, in controlling nociceptive responding. The roles of anandamide and 2-arachidonoylglycerol, released under physiological conditions, in modulating nociceptive responding at different levels of the neuraxis will be emphasized in this review. Effects of modulation of endocannabinoid levels through inhibition of endocannabinoid hydrolysis and uptake is also compared with effects of exogenous administration of synthetic endocannabinoids in acute, inflammatory and neuropathic pain models. Finally, the therapeutic potential of the endocannabinoid signaling system is discussed in the context of identifying novel pharmacotherapies for the treatment of pain.

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Authors: Guindon, J., & Hohmann, A.
Affiliations: University of Georgia (US)
Corresponding author: Hohmann, Andrea
ORCID: Hohmann, Andrea
Venue: CNS & Neurological Disorders - Drug Targets
Publisher: Bentham Science Publishers Ltd.
Published: 2009-12-01
Volume: 8
Issue: 6
Pages: 403-421
ISSN: 1568-007X (ISSN-L)
1871-5273
DOI: 10.2174/187152709789824660
PMC: PMC2834283
OpenAlex: W2054998310
Cited by: 476
References: 255
Citations by year: 2026: 21 · 2025: 19 · 2024: 36 · 2023: 27 · 2022: 41 · 2021: 38 · 2020: 23 · 2019: 25 · 2018: 33 · 2017: 27 · 2016: 23 · 2015: 23 · 2014: 39 · 2013: 28 · 2012: 36
FWCI: 17.25
Type: journal article
Language: en
Open access: green
www.ncbi.nlm.nih.gov
Locations: CNS & Neurological Disorders - Drug Targets (publishedVersion)
PubMed (publishedVersion)
PubMed Central (acceptedVersion)
Funders: National Institute on Drug Abuse (DA022478, DA-022702, R21DA022478, R01DA021644, R21DA022702, DA021644)
Topics: Health Sciences › Medicine › Pharmacology (medical) › Cannabis and Cannabinoid Research
Health Sciences › Medicine › Physiology (medical) › Pain Mechanisms and Treatments
Life Sciences › Neuroscience › Sensory Systems › Ion Channels and Receptors
Keywords: endocannabinoid system, pain, anandamide, 2-arachidonoylglycerol, cannabinoid receptors, CB1 receptor, CB2 receptor, nociception, analgesia, neuropathic pain, inflammatory pain, synthetic cannabinoids, pharmacological pain management
MeSH terms: Animals, Arachidonic Acids, Brain, Glycerides, Humans, Pain, Receptors, Cannabinoid, Polyunsaturated Alkamides, Cannabinoid Receptor Modulators, Endocannabinoids

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The Endocannabinoid System and Pain

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