This study examined the antinociceptive effects of seven imidazoline I 2 receptor ligands in a rat warm water tail withdrawal procedure (46 and 50°C). Agmatine, 2-BFI, phenyzoline, and diphenyzoline produced a significant antinociceptive activity at 46°C. BU224, S22687, and idazoxan had no effect at 46°C up to doses that altered the locomotor activity. None of the drugs showed antinociceptive activity at 50°C. It is suggested that I 2 receptor agonists have antinociceptive activity for acute phasic pain under weak noxious stimulus, and the effects are efficacy-dependent. These data explain the findings that I 2 receptor agonists enhance the antinociceptive effects of opioids and support developing higher-efficacy I 2 receptor agonists for the treatment of pain.

Effects of imidazoline I2 receptor ligands on acute nociception in rats

DEL BELLO, FABIO;
2012-01-01

Abstract

This study examined the antinociceptive effects of seven imidazoline I 2 receptor ligands in a rat warm water tail withdrawal procedure (46 and 50°C). Agmatine, 2-BFI, phenyzoline, and diphenyzoline produced a significant antinociceptive activity at 46°C. BU224, S22687, and idazoxan had no effect at 46°C up to doses that altered the locomotor activity. None of the drugs showed antinociceptive activity at 50°C. It is suggested that I 2 receptor agonists have antinociceptive activity for acute phasic pain under weak noxious stimulus, and the effects are efficacy-dependent. These data explain the findings that I 2 receptor agonists enhance the antinociceptive effects of opioids and support developing higher-efficacy I 2 receptor agonists for the treatment of pain.
2012
262
File in questo prodotto:
Non ci sono file associati a questo prodotto.

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/11581/323787
 Attenzione

Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo

Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 21
  • ???jsp.display-item.citation.isi??? 23
social impact