The novel reversible fatty acid amide hydrolase inhibitor ST4070 increases endocannabinoid brain levels and counteracts neuropathic pain in different animal models (Articolo in rivista)

Type

• Articolo in rivista (Classe)
• Prodotto della ricerca (Classe)

Label

• The novel reversible fatty acid amide hydrolase inhibitor ST4070 increases endocannabinoid brain levels and counteracts neuropathic pain in different animal models (Articolo in rivista) (literal)

Anno

• 2012-01-01T00:00:00+01:00 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi

• 10.1124/jpet.111.191403 (literal)

Alternative label

• Antonio Caprioli 1; Roberto Coccurello 2; Cinzia Rapino 3; Stefano Di Serio 1; Monia Di Tommaso 3; Mario Vertechy 1; Valentina Vacca 2; Natalia Battista 3; Flaminia Pavone 2; Mauro Maccarone 3; Franco Borsini 1 (2012)
  The novel reversible fatty acid amide hydrolase inhibitor ST4070 increases endocannabinoid brain levels and counteracts neuropathic pain in different animal models
  in The Journal of pharmacology and experimental therapeutics (Print)
  (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori

• Antonio Caprioli 1; Roberto Coccurello 2; Cinzia Rapino 3; Stefano Di Serio 1; Monia Di Tommaso 3; Mario Vertechy 1; Valentina Vacca 2; Natalia Battista 3; Flaminia Pavone 2; Mauro Maccarone 3; Franco Borsini 1 (literal)

Pagina inizio

• 188 (literal)

Pagina fine

• 195 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume

• 342 (literal)

Rivista

• ?The ?Journal of pharmacology and experimental therapeutics (Rivista)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#pagineTotali

• 7 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroFascicolo

• 1 (literal)

Note

• PubMe (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni

• 1 Sigma-tau Industrie Farmaceutiche Riunite S.p.A.. 2 Institute of Cell Biology and Neurobiology (IBCN), National Research Council (CNR). 3 Department of Biomedical Sciences. (literal)

Titolo

• The novel reversible fatty acid amide hydrolase inhibitor ST4070 increases endocannabinoid brain levels and counteracts neuropathic pain in different animal models (literal)

Abstract

• The effect of the enol carbamate ST4070 (1-biphenyl-4-ylethenyl piperidine-1-carboxylate), a novel reversible inhibitor of fatty acid amide hydrolase (FAAH), was investigated on acute pain sensitivity and neuropathic pain in rats and mice. Brain enzymatic activity of FAAH and the endogenous levels of its substrates, anandamide (AEA), 2-arachidonoylglycerol (2-AG) and N-palmitoylethanolamine (PEA), were measured in control and ST4070-treated mice. ST4070 (10, 30 and 100 mg/kg) was orally administered to assess mechanical nociceptive thresholds and allodynia using the Randall-Selitto and von Frey tests, respectively. Neuropathy was induced in rats by either the chemotherapeutic agent vincristine or streptozotocin (STZ)-induced diabetes, whilst the chronic constriction injury (CCI) model was chosen to evaluate neuropathy in mice. ST4070 produced a significant increase of nociceptive threshold in rats and counteracted the decrease of nociceptive threshold in the three distinct models of neuropathic pain. In diabetic mice, ST4070 inhibited FAAH activity and increased the brain levels of AEA and PEA, without affecting that of 2-AG. The administration of ST4070 generated a long-lasting pain relief as compared to pregabalin and the FAAH inhibitors OL135 and URB597 in CCI neuropathic mice. The antiallodynic effects of ST4070 were prevented by pretreatment with CB1 and CB2 receptor antagonists as well as by the selective peroxisome proliferator-activated receptor (PPAR)-? antagonist GW6471. The administration of ST4070 generated a long-lasting neuropathic pain relief as compared to pregabalin and the FAAH inhibitors OL135 and URB597. Taken together, the reversible FAAH inhibitor ST4070 appears a promising novel therapeutic agent for the management of neuropathic pain. (literal)

Prodotto di

• ex SV.P16.003.001 / Modelli animali di deficit neurocomportamentale: meccanismi di adattamento a stress - modelli animali (SV.P16.003.004) (Modulo)

Autore CNR

• Valentina Vacca (Persona)
• ROBERTO COCCURELLO (Persona)
• FLAMINIA PAVONE (Unità di personale interno)

Insieme di parole chiave

• Parole chiave di "The novel reversible fatty acid amide hydrolase inhibitor ST4070 increases endocannabinoid brain levels and counteracts neuropathic pain in different animal models" (Insieme di parole chiave)

Incoming links:

Autore CNR di

• FLAMINIA PAVONE (Unità di personale interno)
• ROBERTO COCCURELLO (Persona)
• Valentina Vacca (Persona)

Prodotto

• ex SV.P16.003.001 / Modelli animali di deficit neurocomportamentale: meccanismi di adattamento a stress - modelli animali (SV.P16.003.004) (Modulo)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#rivistaDi

• ?The ?Journal of pharmacology and experimental therapeutics (Rivista)

Insieme di parole chiave di

• Parole chiave di "The novel reversible fatty acid amide hydrolase inhibitor ST4070 increases endocannabinoid brain levels and counteracts neuropathic pain in different animal models" (Insieme di parole chiave)