Atreleuton - CAS 154355-76-7
Catalog number: 154355-76-7
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Leukotriene Receptor | Lipoxygenases (LOXs)
Atreleuton, a kind of urea compound, has been found to be a 5-lipoxygenase inhibitor as well as Leukotriene B4 receptor antagonist that could probably be useful in study of sorts of diseases like asthma and acute coronary syndromes. It has already been discontinued by VIA Pharmaceuticals.
Atreleuton; ABT-761; Atreleuton [USAN]; UNII-U301T88E1M; ABT 761; 1-[(2R)-4-[5-[(4-fluorophenyl)methyl]thiophen-2-yl]but-3-yn-2-yl]-1-hydroxyurea
Store in a cool and dry place and at 0 - 4 °C for short term (days to weeks) or -20 °C for long term (months to years).
Quality Standard:
In-house standard
Canonical SMILES:
1.N-hydroxyurea and hydroxamic acid inhibitors of cyclooxygenase and 5-lipoxygenase.
Connolly PJ;Wetter SK;Beers KN;Hamel SC;Chen RH;Wachter MP;Ansell J;Singer MM;Steber M;Ritchie DM;Argentieri DC Bioorg Med Chem Lett. 1999 Apr 5;9(7):979-84.
Two series of compounds (1 and 2) having structural features of the dual COX/5-LO inhibitor tepoxalin and the 5-LO inhibitor ABT-761 were prepared. Many of these hybrid compounds are potent COX and 5-LO inhibitors; two compounds (1a and 2t) inhibit eicosanoid biosynthesis in an ex vivo assay.
2.Pharmacokinetics of a novel 5-lipoxygenase inhibitor (ABT-761) in pediatric patients with asthma.
Wong SL;Kearns GL;Kemp JP;Drajesk J;Chang M;Locke CS;Dube LM;Awni WM Eur J Clin Pharmacol. 1998 Nov-Dec;54(9-10):715-9.
OBJECTIVE: ;The pharmacokinetics of an N-hydroxyurea analog, ABT-761 in asthmatic pediatric patients with asthma were investigated.;METHODS: ;A total of 24 patients were enrolled into this 8-day single- and multiple-dose study. Patients received daily doses of ABT-761 according to their body weight: patients of 20-38 kg received 50 mg; patients >38 kg but < or = 55 kg received 100 mg, and patients >55 kg received 150 mg.;RESULTS: ;The mean values for the terminal phase t1/2 were 16-17 h after multiple-dose administration. When normalized for body weight, the mean day 8 Cl(f) values for 50-, 100-mg, and 150-mg doses were 0.57 (n=13), 0.51 (n=10), and 0.43 (n=1) ml x min(-1) x kg(-1), respectively, while the mean Vz/f values ranged from 0.75 to 0.77 l x kg(-1). The mean accumulation ratio observed (day 8 to day 1 AUC0-24 ratio) of ABT-761 was approximately 1.7, which is consistent with the t1/2 of this drug. Body weight, age, and body surface area were virtually identical in explaining the variability in dose-normalized Cmax and AUC values (R2=0.61-0.68). The percents of variance explained by these three variables were within a range of 3% for each pharmacokinetic parameter.;CONCLUSIONS: ;The pharmacokinetics of ABT-761 in children were similar to those previously reported in adults.
3.Effects of a 5-lipoxygenase inhibitor, ABT-761, on exercise-induced bronchoconstriction and urinary LTE4 in asthmatic patients.
Lehnigk B;Rabe KF;Dent G;Herst RS;Carpentier PJ;Magnussen H Eur Respir J. 1998 Mar;11(3):617-23.
The novel 5-lipoxygenase (5-LO) inhibitor, ABT-761, was investigated for its effect on exercise-induced bronchoconstriction in asthmatic subjects. The relationship between 5-LO inhibition and effects on the response of the airways to exercise was examined. In a double-blind, randomized, crossover clinical trial, 10 patients with mild to moderate persistent asthma (who exhibited a fall in forced expiratory volume in one second (FEV1) > or = 20% following standardized exercise challenge) received 200 mg ABT-761 or matched placebo, orally, 5 h prior to exercise on two study days, 7-10 days apart. Lung function, urinary leukotriene E4 (LTE4) and ex vivo calcium ionophore-stimulated LTB4 release in whole blood were measured prior to dosing, prior to exercise and at various time points up to 4 h post-exercise. The mean (SD) maximal percentage fall in FEV1 after exercise was 27.1 (12)% on placebo and 19.9 (10)% on ABT-761 days, respectively (p<0.05). Post-exercise fall in FEV1 was significantly attenuated at 5, 10, 15 and 30 min after exercise and the mean area under curve, representing the overall effect of exercise from 0-45 min post-challenge, was also significantly attenuated by ABT-761 (p<0.
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CAS 154355-76-7 Atreleuton

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