Preliminary in vivo testing demonstrated that only the MAGL inhibitor cetirizine influences the nociceptive threshold in laboratory animals.
Therefore, we tested the analgesic efficiency of cetirizine in two animal models of pain:
- osteoarthritic pain induced with Freund's adjuvant (inactivated Koch bacillus)
- pain associated with diabetic neuropathy (streptozotocin-induced diabetes)
Following in vivo evaluation, cetirizine 10 mg/kg decreased pain and heat sensitivity induced by Freund's reagent or streptozotocin. THEREFORE, cetirizine has promising analgesic effect, with in vivo data indicating that it can be used for the treatment of chronic pain in osteoarthritis and diabetic neuropathy.
In addition, cetirizine seems to prevent Freund's adjuvant-induced cartilage loss (confirmation tests are currently being carried out).