生物活性

• 靶点	5-HT Receptor 2B IC50:3.4nM

• 描述PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist that causes selective vasodilation of pulmonary arteries^[5]. In the 5‐HT2B expressing SI‐NET cell line, PRX‐08066 inhibited proliferation (IC50 4.6 × 10⁻⁹M) and 5‐HT secretion (6.9 × 10⁻⁹M) and decreased ERK1/2 phosphorylation and profibrotic growth factor synthesis and secretion, connective tissue growth factor and fibroblast growth factor^[4]. In vitro research suggests that PRX-08066 reduced the population of UM cells in mitosis, impaired their clonogenicity and migration potential, and decreased the phosphorylation of kinases typically activated by HTR2B, as well as new targets such as β-catenin, PYK2 and STAT5^[5]. In vivo research shows the 5-HT2BR antagonist PRX-08066 reduced monocrotaline-induced pulmonary arterial hypertension and right ventricular hypertrophy in rats^[6].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT00345774	Pulmonary Hypertension ... more >> Chronic Obstructive Pulmonary Disease Collapse <<	Phase 2	Completed	-	United States, Alabama ... more >> Pinnacle Research Group, LLC Anniston, Alabama, United States, 36207 United States, Arizona Arizona Pulmonary Specialists, Ltd. Phoenix, Arizona, United States, 85013 United States, California University of California-Davis Medical Group Sacramento, California, United States, 95817 United States, Florida University Clinical Research-DeLand, LLC DeLand, Florida, United States, 32720 Central Medical Group, PA Tamarac, Florida, United States, 33321 Clinical Research of West Florida, Inc. Tampa, Florida, United States, 33603 United States, Georgia Atlanta Insitute for Medical Research Decatur, Georgia, United States, 30030 United States, Idaho Pulmonary Consultants of North Idaho Coeur d'Alene, Idaho, United States, 83814 United States, Illinois Loyola University Medical Center Foster McGraw Hospital Maywood, Illinois, United States, 60153 United States, Kansas Veritas Clinical Specialities Topeka, Kansas, United States, 66606 United States, Massachusetts Tufts New England Medical Center Boston, Massachusetts, United States, 02111 Massachusetts General Hospital, Pulmonary Critical Care Unit Boston, Massachusetts, United States, 02114 United States, New York Buffalo Cardiology and Pulmonary Associates, P.C. Williamsville, New York, United States, 14221 United States, North Carolina American Health Research Charlotte, North Carolina, United States, 28207 United States, South Carolina South Carolina Pharmaceutical Research Spartanburg, South Carolina, United States, 29303 Spartanburg Medical Research Spartanburg, South Carolina, United States, 29303 United States, Texas Baylor College of Medicine Houston, Texas, United States, 77030 United States, West Virginia Morgantown Pulmonary Clinical Research Morgantown, West Virginia, United States, 26505 United States, Wisconsin Heart Care Associates, LLC Milwaukee, Wisconsin, United States, 53215 Collapse <<
  NCT00677872	COPD Pulmonar... more >>y Hypertension Collapse <<	Phase 2	Terminated	-	United States, Massachusetts ... more >> Massachusetts General Hospital Pulmonary and Critical Care Unit Boston, Massachusetts, United States, 02114 Collapse <<