Antrafenine

Antrafenine (Stakane) is a derivative of 2-(quinolin-4-ylamino) benzoate, and is an orally active anti-inflammatory and analgesic agent. Antrafenine protects mammalian epithelial cells from cell death upon exposure to influenza A virus A/WSN/33 (H1N1). Antrafenine inhibits carrageenan-induced paw swelling in rats, and reduces exudate volume and total leukocyte infiltration in carrageenan- and calcium pyrophosphate dihydrate crystal-induced pleurisy in rats. Antrafenine can be used in studies related to influenza and pseudogout^[1][2]. In Vitro:Antrafenine (compound 38) (100 μM; 24 hours-2 days) shows weak cytopathic protection but minimal virus inhibitory activity against influenza A/WSN/33 (H1N1) in MDCK cells, with no significant inhibition observed at 100 μM^[1]. In Vivo:Antrafenine (10-40 mg/kg; p.o.; single dose) suppresses carrageenan-induced paw oedema in male CD Sprague Dawley rats with an ED₄₀ of 24 mg/kg p.o., achieving up to 55% reduction at 40 mg/kg p.o^[2].
Antrafenine (10-40 mg/kg; p.o.; single dose) suppresses carrageenan-induced pleurisy in male CD Sprague Dawley rats, with an ED₄₀ of 15 mg/kg p.o. for exudate volume reduction and 33 mg/kg p.o. for leucocyte infiltration reduction^[2].
Antrafenine (10-40 mg/kg; p.o.; single dose) suppresses calcium pyrophosphate dihydrate crystal-induced pleurisy in male CD Sprague Dawley rats, with an ED₄₀ of 20 mg/kg p.o. for exudate volume reduction and 40 mg/kg p.o. for leucocyte infiltration reduction^[2].
Antrafenine (200-400 mg/kg; p.o.; single dose) exhibits mild acute ulcerogenic activity in fasted male CD Sprague Dawley rats at oral doses of 200 and 400 mg/kg, with mean ulcer scores of 0.58 and 0.65 respectively and no mortality^[2].