Nitroparacetamol exhibits anti-inflammatory and anti-nociceptive activity.
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.
al-Swayeh
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OA
Department of Medicine, King Saud University, Riyadh, Kingdom of Saudi Arabia.
Futter
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LE
Clifford
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RH
Moore
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PK
D000082:Acetaminophen / Q000031:analogs & derivatives / Q000627:therapeutic use; D000700:Analgesics / Q000627:therapeutic use*; D000704:Analysis of Variance; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000627:therapeutic use*; D002351:Carrageenan; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control*; D008297:Male; D010146:Pain / Q000517:prevention & control*; D010147:Pain Measurement / Q000187:drug effects; D051381:Rats; D017208:Rats, Wistar
D000700:Analgesics; D000893:Anti-Inflammatory Agents; D000082:Acetaminophen; D002351:Carrageenan