Atreleuton is an inhibitor of 5-lipoxygenase (5-LO; IC50 = 23 nM in rat basophil leukemia cell lysates).1 It inhibits leukotriene B4 formation induced by A23187 in isolated human whole blood (IC50 = 160 nM). Atreleuton inhibits LTE4 and LTB4 biosynthesis in the peritoneal cavity in a rat model of anaphylaxis (ED50s = 1.4 and 0.6 mg/kg, respectively) and bronchoconstriction induced by arachidonic acid in anesthetized guinea pigs (ED50 = 3 mg/kg).2
1.Brooks, C.D., Stewart, A.O., Basha, A., et al.(R)-(+)-N-[3-[5-[(4-fluorophenyl)methyl]-2-thienyl]-1-methyl- 2-propynyl]-N-hydroxyurea (ABT-761), a second-generation 5-lipoxygenase inhibitorJ. Med. Chem.38(24)4768-4778(1995) 2.Bell, R.L., Harris, R.R., Malo, P.E., et al.ABT-761 attenuates bronchoconstriction and pulmonary inflammation in rodentsJ. Pharmacol. Exp. Ther.280(3)1366-1373(1997)