URB597, an inhibitor of fatty acid amide hydrolase, reduces hyperalgesia in diabetic rats
Abstract
Diabetic rats display increased pain responses after injection of formalin into the paw or thermal stimulation of the tail, suggesting the presence of hyperalgesia. In this study, we investigated the efficacy of URB597 (0.1, 0.3, and 0.5 mg/kg, i.p.), an inhibitor of endocannabinoids metabolism, on 2 models of experimental hyperalgesia in streptozotocin (STZ)-induced diabetic rats. Animals were divided into control, URB597-treated control (0.1, 0.3, and 0.5 mg/kg), diabetic, and URB597-treated diabetic (0.1, 0.3, and 0.5 mg/kg) groups. Formalin and tail-flick tests were performed 4 and 8 weeks after the onset of hyperglycemia, respectively. Diabetes caused significant hyperalgesia during these tests. URB597 (0.3 and 0.5 mg/kg) reversed chemical and thermal hyperalgesia in diabetic rats. Administration of URB597 at a dose of 0.1 mg/kg did not alter pain-related behaviors in control and diabetic groups compared with those of the respective control groups. URB597 treatment did not affect body weight or plasma glucose level of treated animals compared with nontreated animals. This study shows that increasing endocannabinoid neurotransmission with URB597 displays efficacy in chemical and thermal models of diabetic hyperalgesia. It also suggests that URB597 is a promising tool for treatment of painful diabetic neuropathy.
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FAAH and MAGL inhibitors reduce nociceptive behavior in STZ-injected rats.
“In addition, FAAH (Hasanein et al, 2009;Sasso et al, 2015) and MAGL (Niphakis et al, 2013) inhibitors reduce nociceptive behavior in STZ-injected rats.”
From The endogenous cannabinoid system: a budding source of targets for treating inflammatory and neuropathic pain (2018) · cites this paper as Hasanein et al, 2009
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Self-citation
- Authors
- Hasanein, P., Parviz, M., Keshavarz, M., & Roohbakhsh, A.
- Affiliations
- Bu-Ali Sina University (IR)
- Venue
- Canadian Journal of Physiology and Pharmacology
- Publisher
- Canadian Science Publishing
- Published
- 2009-06
- Volume
- 87
- Issue
- 6
- Pages
- 432-439
- ISSN
- 0008-4212 (ISSN-L)
- 1205-7541
- OpenAlex
- W2019815408
- Cited by
- 14
- References
- 46
- Citations by year
- 2024: 1 · 2023: 1 · 2021: 2 · 2019: 1 · 2018: 1 · 2017: 1 · 2015: 1 · 2014: 4 · 2013: 1
- FWCI
- 0.22
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Canadian Journal of Physiology and Pharmacology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Physiology › Pain Mechanisms and Treatments
- Health Sciences › Medicine › Pharmacology › Cannabis and Cannabinoid Research
- Life Sciences › Neuroscience › Sensory Systems › Ion Channels and Receptors
- Keywords
- URB597, fatty acid amide hydrolase inhibition, endocannabinoids, diabetic neuropathic pain, formalin test, tail-flick test, thermal hyperalgesia, streptozotocin-induced diabetes
- MeSH terms
- Fatty Acid Amide Hydrolases, Amidohydrolases, Animals, Benzamides, Blood Glucose, Body Weight, Carbamates, Diabetes Mellitus, Experimental, Dose-Response Relationship, Drug, Enzyme Inhibitors, Hyperalgesia, Injections, Intraperitoneal, Male, Pain Measurement, Temperature, Rats, Wistar, Pain Threshold, Rats, Cannabinoid Receptor Modulators
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