1. Effects of a selective sigma 1 antagonist compound on inflammatory pain.
- Author
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Parenti C, Marrazzo A, Aricò G, Cantarella G, Prezzavento O, Ronsisvalle S, Scoto GM, and Ronsisvalle G
- Subjects
- Animals, Carrageenan, Cyclopropanes pharmacology, Disease Models, Animal, Edema chemically induced, Hyperalgesia chemically induced, Inflammation chemically induced, Male, Nitric Oxide metabolism, Nitric Oxide Synthase metabolism, Pain chemically induced, Pain Measurement, Rats, Rats, Sprague-Dawley, Edema drug therapy, Hyperalgesia drug therapy, Inflammation drug therapy, Pain drug therapy, Receptors, sigma antagonists & inhibitors
- Abstract
The compound (−)-MRV3 [(−)-Methyl (1S,2R)-2-[(4-Hydroxy-4-phenylpiperidin-1-yl)-methyl]-1-phenylcyclopropanecarboxylate] has an assessed antagonistsigma 1 (σ1) profile and showed improved σ1/σ2 selectivity with respect to the parent compound(+)-MR200. The σ1 receptor is reported to play arole in both central sensitization and pain hypersensitivity,which suggests a potential use of σ1 antagonists forthe treatment of persistent pain conditions. The present study was performed to assess the effects of theselective σ1 antagonist (−)-MRV3, in carrageenan-inducedinflammatory hyperalgesia, allodynia and edema.Mechanical allodynia with a series of calibratedvon Frey’s filaments, thermal hyperalgesia with plantartest and edema evaluation with a plethysmometerwere measured. Subcutaneous (s.c.) treatment with(−)-MRV3 (1, 2, 3, 4, 5 mg/kg) dose-dependentlyreduced allodynia and hyperalgesia induced byintraplantar carageenan. Furthermore, treatment with(−)-MRV3 (3 mg/kg s.c.) also inhibited paw edemawith a significant inhibition of 61.53 % 3 h aftercarrageenan treatment [corrected]. These results provide a strongbasis for the use of σ1 receptor antagonists in thetreatment of inflammatory pain.
- Published
- 2014
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