Nitroparacetamol exhibits anti-inflammatory and anti-nociceptive activity.

Abstract

Nitroparacetamol (NCX-701) is a newly synthesized nitric oxide-releasing derivative of paracetamol. Following i.p. administration, nitroparacetamol inhibits carrageenan-induced hindpaw oedema formation (ED(50), 169.4 micromol kg(-1)) and mechanical hyperalgesia (ED(50), 156 micromol kg(-1)) in the rat. In contrast, the parent compound, paracetamol, exhibits no significant anti-oedema activity in this model (ED(50)>1986 micromol kg(-1), i.p. ) and is markedly less potent than nitroparacetamol as an inhibitor of carrageenan-mediated hyperalgesia (ED(50), 411.6 micromol kg(-1), i.p.). In a second model of nociception (inhibition of acetic acid induced abdominal constrictions in the mouse), nitroparacetamol administered orally (ED(50), 24.8 micromol kg(-1)), was again considerably more potent than paracetamol (ED(50), 506 micromol kg(-1), p.o.). Thus, compared with paracetamol, nitroparacetamol not only exhibits augmented antinociceptive activity in both rat and mouse but, intriguingly, is also anti-inflammatory over a similar dose range.

• Authors: O A al-Swayeh, L E Futter, R H Clifford, P K Moore
• Journal: British journal of pharmacology (Br J Pharmacol) Vol. 130 Issue 7 Pg. 1453-6 (Aug 2000) ISSN: 0007-1188 [Print] England
• PMID: 10928944 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Analgesics
• Anti-Inflammatory Agents
• Acetaminophen
• Carrageenan

Topics

• Acetaminophen (analogs & derivatives, therapeutic use)
• Analgesics (therapeutic use)
• Analysis of Variance
• Animals
• Anti-Inflammatory Agents (therapeutic use)
• Carrageenan
• Edema (chemically induced, prevention & control)
• Male
• Pain (prevention & control)
• Pain Measurement (drug effects)
• Rats
• Rats, Wistar