The compound (-)-MRV3 [(-)-methyl (1S,2R)-2-[(4-hydroxy-4-phenylpiperidin-1-yl)-methyl]-1-phenylcyclopropanecarboxylate] has an assessed antagonist sigma 1 (σ1) profile and showed improved σ1/σ2 selectivity with respect to the parent compound (+)-MR200. The σ1 receptor is reported to play a role in both central sensitization and pain hypersensitivity, which suggests a potential use of σ 1 antagonists for the treatment of persistent pain conditions. The present study was performed to assess the effects of the selective σ1 antagonist (-)-MRV3, in carrageenan-induced inflammatory hyperalgesia, allodynia, and edema. Mechanical allodynia with a series of calibrated von Frey's filaments, thermal hyperalgesia with plantar test, and edema evaluation with a plethysmometer were measured. Subcutaneous (s.c.) treatment with (-)-MRV3 (1, 2, 3, 4, 5 mg/kg) dose-dependently reduced allodynia and hyperalgesia induced by intraplantar carrageenan. Furthermore, treatment with (-)-MRV3 (3 mg/kg s.c.) also inhibited paw edema with a significant inhibition of 37.82 % 3 h after carrageenan treatment. These results provide a strong basis for the use of σ1 receptor antagonists in the treatment of inflammatory pain

Effects of a Selective Sigma 1 Antagonist Compound on Inflammatory Pain

Parenti Carmela;Marrazzo Agostino;Aricò Giuseppina;Cantarella Giuseppina;Prezzavento Orazio;Ronsisvalle Simone;Scoto Giovanna Maria;
2014-01-01

Abstract

The compound (-)-MRV3 [(-)-methyl (1S,2R)-2-[(4-hydroxy-4-phenylpiperidin-1-yl)-methyl]-1-phenylcyclopropanecarboxylate] has an assessed antagonist sigma 1 (σ1) profile and showed improved σ1/σ2 selectivity with respect to the parent compound (+)-MR200. The σ1 receptor is reported to play a role in both central sensitization and pain hypersensitivity, which suggests a potential use of σ 1 antagonists for the treatment of persistent pain conditions. The present study was performed to assess the effects of the selective σ1 antagonist (-)-MRV3, in carrageenan-induced inflammatory hyperalgesia, allodynia, and edema. Mechanical allodynia with a series of calibrated von Frey's filaments, thermal hyperalgesia with plantar test, and edema evaluation with a plethysmometer were measured. Subcutaneous (s.c.) treatment with (-)-MRV3 (1, 2, 3, 4, 5 mg/kg) dose-dependently reduced allodynia and hyperalgesia induced by intraplantar carrageenan. Furthermore, treatment with (-)-MRV3 (3 mg/kg s.c.) also inhibited paw edema with a significant inhibition of 37.82 % 3 h after carrageenan treatment. These results provide a strong basis for the use of σ1 receptor antagonists in the treatment of inflammatory pain
2014
hyperalgesia; allodynia; sigma 1 receptor; edema; carrageenan
File in questo prodotto:
File Dimensione Formato  
Inflammation 2013 PDF.pdf

solo gestori archivio

Licenza: Non specificato
Dimensione 207.06 kB
Formato Adobe PDF
207.06 kB Adobe PDF   Visualizza/Apri

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.11769/53641
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 21
  • ???jsp.display-item.citation.isi??? 21
social impact