A new sigma ligand, (+/-)-PPCC, antagonizes kappa opioid receptor-mediated antinociceptive effect

The compound (1R,2S/1S,2R)-2-[4-hydroxy-4-phenylpiperidin-1-yl)methyl]-1-(4-methylphenyl) cyclopropanecarboxylate [(+/-)-PPCC] is a ligand with high affinity for sigma (sigma) sites of which the selectivity towards several other receptor systems has been demonstrated. Given the existence of a relationship between the sigma system and the kappa opioid (KOP)-mediated analgesia, to characterize the pharmacological properties of (+/-)-PPCC we analyzed its influence on the analgesic effect of the systemic injected kappa agonist (-)-U-50,488H comparing the effects with those shown by (+)-pentazocine and BD1047. The results demonstrate that the systemic administration of (+/-)-PPCC (1 mg/kg s.c.) does not modify basal tail-flick latency. Pre-treatment with (+/-)-PPCC, at the same dose, significantly decreased the antinociceptive effect of (-)-U-50,488H, analogously to the sigma compounds used. This study confirms that (+/-)-PPCC plays the role of sigma agonist in this model and strengthens the hypothesis of the sigma receptor modulatory role on KOP-mediated analgesia.

A new sigma ligand, (+/-)-PPCC, antagonizes kappa opioid receptor-mediated antinociceptive effect / PREZZAVENTO O; PARENTI C; MARRAZZO A; RONSISVALLE S; VITTORIO F; ARICÒ G; SCOTO GM; RONSISVALLE G. - In: LIFE SCIENCES. - ISSN 0024-3205. - 82(2008), pp. 549-553.

Titolo: A new sigma ligand, (+/-)-PPCC, antagonizes kappa opioid receptor-mediated antinociceptive effect
Autori interni: 
PREZZAVENTO, Orazio
PARENTI, Carmela
MARRAZZO, Agostino
RONSISVALLE, SIMONE
SCOTO, Giovanna Maria
RONSISVALLE, Giuseppe
mostra contributor esterni 
Data di pubblicazione: 2008
Rivista: 
LIFE SCIENCES  
Citazione: A new sigma ligand, (+/-)-PPCC, antagonizes kappa opioid receptor-mediated antinociceptive effect / PREZZAVENTO O; PARENTI C; MARRAZZO A; RONSISVALLE S; VITTORIO F; ARICÒ G; SCOTO GM; RONSISVALLE G. - In: LIFE SCIENCES. - ISSN 0024-3205. - 82(2008), pp. 549-553.
Handle: http://hdl.handle.net/20.500.11769/5723
Appare nelle tipologie:1.1 Articolo in rivista

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