FPL 62064, a topically active 5-lipoxygenase/cyclooxygenase inhibitor.
FLP 62064 [N-(4-methoxyphenyl)-1-phenyl-1H-pyrazole-3-amine] is a dual inhibitor of prostaglandin synthetase and 5-lipoxygenase. The compound had anti-inflammatory activity in vivo in a number of models. It inhibited peritoneal inflammation induced by immune-complex when given locally. When applied to the skin, FPL 62064 inhibited UV irradiation-induced erythema and PGE2 formation in the guinea pig and also oedema formation and eicosanoid production in the mouse ear produced by arachidonic acid. Co-injected with arachidonic acid in rabbit skin, FPL 62064 inhibited oedema and eicosanoid formation.
Blackham
A
A
Department of Biochemistry, Fisons plc-Pharmaecutical Division, Loughborough, Leicestershire, UK.
Griffiths
R J
RJ
Hallam
C
C
Mann
J
J
Mitchell
P D
PD
Norris
A A
AA
Simpson
W T
WT
D000279:Administration, Cutaneous; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D000936:Antigen-Antibody Complex; D001091:Arachidonate Lipoxygenases / Q000037:antagonists & inhibitors*; D016718:Arachidonic Acid; D001095:Arachidonic Acids; D002351:Carrageenan; D016861:Cyclooxygenase Inhibitors; D015777:Eicosanoids / Q000378:metabolism; D005260:Female; D006168:Guinea Pigs; D006801:Humans; D066298:In Vitro Techniques; D007249:Inflammation / Q000188:drug therapy / Q000209:etiology; D016859:Lipoxygenase Inhibitors; D051379:Mice; D009504:Neutrophils / Q000201:enzymology; D015230:Prostaglandin D2 / Q000032:analysis; D011720:Pyrazoles / Q000494:pharmacology*; D011817:Rabbits; D013755:Tetradecanoylphorbol Acetate; D014466:Ultraviolet Rays
D000894:Anti-Inflammatory Agents, Non-Steroidal; D000936:Antigen-Antibody Complex; D001095:Arachidonic Acids; D016861:Cyclooxygenase Inhibitors; D015777:Eicosanoids; D016859:Lipoxygenase Inhibitors; D011720:Pyrazoles; C065337:FPL 62064; D016718:Arachidonic Acid; D002351:Carrageenan; D001091:Arachidonate Lipoxygenases; D013755:Tetradecanoylphorbol Acetate; D015230:Prostaglandin D2