货号：A202709同义名：
齐留通(Zileuton)
/ A 64077;Abbott 64077
Zileuton is a reversible 5-lipoxygenase inhibitor with IC50 value of 0.5 µM in rat basophilic leukemia-1 (RBL-1) cells. It also potently inhibited leukotriene B4 production with an IC50 value of 0.6 µM in purified human peripheral blood polymorphonuclear leukocytes (PMNL).
Leukotrienes (LT) are metabolites of arachidonic acid (AA) formed from the 5-lipoxygenase (5-LOX) pathway. They exhibit a number of biological effects such as contraction of smooth muscles, especially bronchoconstriction, increased vascular permeability, and migration of leukocytes to areas of inflammation. Zileuton is a potent and selective inhibitor of 5-lipoxygenase with antiasthmatic properties[3]. In macrophages, zileuton overinterfered with arachidonic acid (AA) release to inhibit PG biosynthesis. In activated mouse peritoneal macrophages and macrophage J774, zileuton significantly reduces PGE2 and 6-ketone prostaglandin F1α (PGF1α) levels[4]. In anti-CD3-treated cells, IL-2 decreased in zileuton-treated and untreated cells with increasing incubation time. Zileuton likely reduced IL-2 levels by inhibiting 5-lipoxygenase[3]. Zileuton treatement on rats with TNB colitis, however, showed a significant reduction in the macroscopic damage score after four weeks of treatment compared with 5-ASA and placebo groups. The intracolonic administration of 50 mg/kg of zileuton after colitis induction decreased the local peak release of LTB4 by 90%[5]. In zileuton (5 mg/kg, p.o.) treated ischemia/reperfusion (I/R) rat, the effect of zileuton to decrease NF-κB expression did not change significantly in the presence of COX inhibitors, and the group revealed significantly lower level of NF-κB staining. Zileuton (5 mg/kg, p.o.) treatment given to I/R rats decreased apoptotic index significantly. In 5-LOX gene knockout mice, administration of zileuton before I/R significantly reduced the degree of renal dysfunction (urea, creatinine) and injury (AST, histology). In addition, zileuton reduced the expression of ICAM-1 and the associated polymorphonuclear leukocyte infiltration caused by I/R of the mouse kidney[6]. Although zileuton inhibited LTB4 production in the peritonitis model more effectively than the LTA4H inhibitor, the influx of neutrophils into the peritoneum after 1 and 2h was significantly higher in zileuton- versus JNJ-26993135-treated animals[7].
United States, Maryland
... 展开 >>
Pfizer Investigational Site
Baltimore, Maryland, United States, 21225
United States, Massachusetts
Pfizer Investigational Site
North Dartmouth, Massachusetts, United States, 02747
United States, Michigan
Pfizer Investigational Site
Kalamazoo, Michigan, United States, 49007
United States, Nebraska
Pfizer Investigational Site
Omaha, Nebraska, United States, 68131 收起 <<
United States, California
... 展开 >>
Allergy & Asthma Specialist Medical Group
Huntington Beach, California, United States, 92647
Allergy and Asthma Medical Group and Research Center
San Diego, California, United States, 92123
United States, Colorado
Colorado Allergy and Asthma Centers, PC
Englewood, Colorado, United States, 80112
United States, Massachusetts
Northeast Medical Research Associates
North Dartmouth, Massachusetts, United States, 02747
United States, Minnesota
Clinical Research Institute
Minneapolis, Minnesota, United States, 55402
United States, Missouri
The Clinical Research Center, L.L.C.
St. Louis, Missouri, United States, 63141
United States, New Jersey
Princeton Center for Clinical Research
Skillman, New Jersey, United States, 08558
United States, Ohio
Bernstein Clinical Research Center
Cincinnati, Ohio, United States, 45231
United States, Oregon
Allergy Associates Research Center
Portland, Oregon, United States, 97213
United States, Texas
Western Sky Medical Research
El Paso, Texas, United States, 79902 收起 <<
Terminated(Lack of feasibility... 展开 >> due to low recruitment) 收起 <<
-
United States, Alabama
... 展开 >>
University of Alabama Lung Health Center
Birmingham, Alabama, United States, 35249
Veteran's Administration Medical Center
Birmingham, Alabama, United States, 35294
United States, California
LA BioMed at Harbor, University of California
Los Angeles, California, United States, 90502
University of California San Francisco-Airway Clinical Research Center
San Francisco, California, United States, 94143
United States, Colorado
Denver Health Medical Center
Denver, Colorado, United States, 80204
National Jewish Medical and Research Center
Denver, Colorado, United States, 80206
Veteran's Administration Medical Center
Denver, Colorado, United States, 80220
United States, Maryland
University of Maryland Hospital
Baltimore, Maryland, United States, 21201
United States, Massachusetts
Fallon Clinic
Boston, Massachusetts, United States, 01605
Brigham and Women's Hospital
Boston, Massachusetts, United States, 02115
Veteran's Administration Medical Center
Boston, Massachusetts, United States, 02132
United States, Michigan
Veteran's Administration Medical Center
Ann Arbor, Michigan, United States, 48105
University of Michigan Medical Center
Ann Arbor, Michigan, United States, 48109
United States, Minnesota
Veteran's Administration Medical Center
Minneapolis, Minnesota, United States, 55417
HealthPartners Research Foundation
Minneapolis, Minnesota, United States, 55440
Mayo Clinic
Rochester, Minnesota, United States, 55905
United States, Pennsylvania
Temple University Lung Center
Philadelphia, Pennsylvania, United States, 19140
University of Pittsburgh Emphysema Research Center
Pittsburgh, Pennsylvania, United States, 15213 收起 <<
United States, California
... 展开 >>
Therapeutics Clinical Research
San Diego, California, United States, 92123
United States, Georgia
MedaPhase, Inc.
Newnan, Georgia, United States, 30263
United States, Kentucky
Dermatology Specialists, PSC
Louisville, Kentucky, United States, 40202
United States, Minnesota
Minnesota Clinical Study Center
Fridley, Minnesota, United States, 55432
United States, New Mexico
Academic Dermatology Associates
Albuquerque, New Mexico, United States, 87106
United States, New York
SUNY Downstate Medical Center
Brooklyn, New York, United States, 11203
Dermatology Associates of Rochester
Rochester, New York, United States, 14623
United States, Pennsylvania
Milton S. Hersey Medical Center
Hersey, Pennsylvania, United States, 17033-0850
United States, Tennessee
Rivergate Dermatology
Goodlettsville, Tennessee, United States, 37072
United States, Texas
DermResearch, Inc.
Austin, Texas, United States, 78759
J&S Studies, Inc.
Bryan, Texas, United States, 77802
United States, Virginia
Virginia Clinical Research, Inc.
Norfolk, Virginia, United States, 23507 收起 <<
United States, New York
... 展开 >>
Weill Cornell Medical College in New York City, Cornell University
New York, New York, United States, 10021
United States, Texas
MD Anderson Cancer Center - Consortium Lead Organzation
Houston, Texas, United States, 77030 收起 <<
Current Every Day Smoker
... 展开 >> Multiple Pulmonary Nodules
Tobacco Smoking
Tobacco Use Disorder 收起 <<
Phase 2
Recruiting
-
United States, Arizona
... 展开 >>
The University of Arizona Medical Center-University Campus
Recruiting
Tucson, Arizona, United States, 85724
Contact: Linda L. Garland 520-626-3434 lgarland@azcc.arizona.edu
Principal Investigator: Linda L. Garland
United States, California
University of California Davis Comprehensive Cancer Center
Recruiting
Sacramento, California, United States, 95817
Contact: Jun Yan 530-752-5109 junyang@ucdavis.edu
Principal Investigator: Jun Yan
United States, Massachusetts
Boston University School of Medicine
Recruiting
Boston, Massachusetts, United States, 02118
Contact: Avrum Spira 617-414-6960 aspira@bu.edu
Principal Investigator: Avrum Spira 收起 <<
搜索
