Nitroparacetamol exhibits anti‐inflammatory and anti‐nociceptive activity

Autor: Al‐Swayeh, O A, Futter, L E, Clifford, R H, Moore, P K
Zdroj: British Journal of Pharmacology; August 2000, Vol. 130 Issue: 7 p1453-1456, 4p
Abstrakt: Nitroparacetamol (NCX‐701) is a newly synthesized nitric oxide‐releasing derivative of paracetamol. Following i.p. administration, nitroparacetamol inhibits carrageenan‐induced hindpaw oedema formation (ED50, 169.4 μmol kg−1) and mechanical hyperalgesia (ED50, 156 μmol kg−1) in the rat. In contrast, the parent compound, paracetamol, exhibits no significant anti‐oedema activity in this model (ED50>1986 μmol kg−1, i.p.) and is markedly less potent than nitroparacetamol as an inhibitor of carrageenan‐mediated hyperalgesia (ED50, 411.6 μmol kg−1, i.p.). In a second model of nociception (inhibition of acetic acid induced abdominal constrictions in the mouse), nitroparacetamol administered orally (ED50, 24.8 μmol kg−1), was again considerably more potent than paracetamol (ED50, 506 μmol 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.
Databáze: Supplemental Index