"目录号: HY-14136
Rimonabant(SR141716)是中心CB1受体反向激动剂，Ki为1.8 nM。
相关产品
WIN 55,212-2 Mesylate-AM251-Rimonabant Hydrochloride-Taranabant-AM630-Org 27569-Otenabant-Pregnenolone-A-836339-CB1-IN-1-JWH-133-Bay 59-3074-BML-190-JD-5037-(±)-SLV319-
生物活性
Description
Rimonabant(SR141716) is a selective central cannabinoid (CB1) receptor inverse agonist with Ki of 1.8 nM.IC50 Value: 1.8 nM(Ki)Target: CB1 Receptorin vitro: Rimonabant dose-dependently reduces ACAT activity in Raw264.7macrophages with IC50 of 2.9 μM and isolated peritoneal macrophages. Rimonabant inhibits ACATactivity in intact CHO-ACAT1 and CHO-ACAT2 cells and in cell-free assays with approximately equal efficiency with IC50 of 1.5 μM and 2.2 μM for CHO-ACAT1 and CHO-ACAT2, respectively. Consistent with ACAT inhibition, Rimonabant treatment blocks ACAT dependent processes in macrophages, oxysterol-induced apoptosis and acetylated-LDL induced foam cell formation. Rimonabant antagonizes the inhibitory effects of cannabinoid receptor agonists on both mouse vas deferens contractions and adenylyl cyclase activity in rat brain membranes in a concentration-dependent manner.in vivo: Rimonabant (10 mg/kg by gavage) is fed for 2 weeks to 3-month-old male obese Zucker rats as an impaired glucose tolerance model and for 10 weeks to 6-month-old male obese Zucker rats as a model of the metabolic syndrome. RANTES (Regulated upon Activation, Normal T cell Expressed, and Secreted) and MCP-1 (monocyte chemotactic protein-1) serum levels are increased in obese vs lean Zucker rats and significantly reduced by long-term treatment with Rimonabant, which slowes weight gain in rats with the metabolic syndrome. Neutrophils and monocytes are significantly increased in young and old obese vs lean Zucker rats and lowered by Rimonabant. Platelet-bound fibrinogen is significantly enhanced in obese vs lean Zucker rats of both age, and is reduced by Rimonabant. Platelets from obese rats are more sensitive to thrombin-induced aggregation and adhesion to fibrinogen, which are both attenuated by Rimonabant therapy.
Clinical Trial
Sanofi
Cardiovascular Disease
December 2005
Phase 3
Sanofi
Carotid Artery Plaque-Arteriosclerosis-Obesity-Metabolic Syndrome X
August 2005
Phase 3
Sanofi
Fatty Liver
January 2008
Phase 3
Sanofi
Fatty Liver
February 2008
Phase 3
University of Surrey-European Foundation for the Study of Diabetes-Royal Surrey County Hospital
Obesity
July 2007
Phase 4
Sanofi
Prediabetic State
May 2006
Phase 3
Sanofi
Metabolic Syndrome
February 2006
Phase 3
University of Maryland-National Institute on Drug Abuse (NIDA)
Schizophrenia-Schizoaffective Disorder-Obesity-Hypertension-Smoking
November 2007
Phase 2
Sanofi
Diabetes Mellitus, Type 2
May 2008
Phase 3
Weill Medical College of Cornell University-National Institutes of Health (NIH)-PWSAUSA
Prader-willi Syndrome
August 2007
Phase 3
Sanofi
Obesity-Diabetes Mellitus Type 2
April 2007
Phase 3
Sanofi
Diabetes Mellitus, Type 2
September 2008
Phase 3
Sanofi
Obesity-Diabetes Mellitus Type 2
April 2007
Phase 3
Sanofi
Diabetes Mellitus, Type 2
March 2007
Phase 3
Sanofi
Smoking Cessation
April 2004
Phase 3
Sanofi
Smoking Cessation
November 2002
Phase 3
Sanofi
Diabetes Mellitus, Type 2
October 2007
Phase 3
Sanofi
Smoking Cessation
September 2002
Phase 3
Sanofi
Obesity
December 2006
Phase 3
Sanofi
Obesity-Microalbuminuria-Diabetes Mellitus, Type 2-Dyslipidemia
March 2007
Phase 3
Sanofi
Obesity-Dyslipidemias
December 2006
Phase 3
Sanofi
Maintenance of Smoking Cessation
November 2002
Phase 3
National Institute on Alcohol Abuse and Alcoholism (NIAAA)-Sanofi-Synthelabo-National Institutes of Health Clinical Center (CC)
Healthy-Alcohol Drinking
December 31, 2003
Phase 2
Sanofi
Obesity-Eating Disorders
August 2004
Phase 3
Sanofi
Obesity-Weight Loss
April 2008
Phase 3
Sanofi
Obesity
October 2004
Phase 2
Sanofi
Smoking Cessation
September 2004
Phase 3
University Hospital, Clermont-Ferrand
Pain
September 2008
Phase 1
Sanofi
Dyslipidemia-Obesity
May 2005
Phase 3
Sanofi
Obesity
May 2004
Phase 3
Sanofi
Obesity
October 2001
Phase 3
Sanofi
Coronary Atherosclerosis
January 2005
Phase 3
Sanofi
Obesity
October 2006
Phase 3
Sanofi
Type 2 Diabetes Mellitus
March 2005
Phase 3
Sanofi
Obesity
February 2007
Phase 3
Sanofi
Type 2 Diabetes Mellitus
January 2006
Phase 3
Sanofi
Obesity
April 2006
Phase 3
National Institute on Drug Abuse (NIDA)-National Institutes of Health Clinical Center (CC)
Cannabis-Dependence
April 16, 2006
Phase 1
The Scripps Research Institute-National Institute on Drug Abuse (NIDA)
Cannabis Dependence-Cannabis Withdrawal
April 30, 2008
Phase 2
Sanofi
Obesity-Weight Loss
August 2001
Phase 3
Sanofi
Obesity-Diabetes Mellitus, Non-Insulin-Dependent-Obesity in Diabetes
October 2001
Phase 3
Sanofi
Obesity-Dyslipidemia
September 2001
Phase 3
Hospital Arnau de Vilanova-Pfizer
Atherosclerosis-Cardiovascular Diseases
April 2008
Phase 4
Aristotle University Of Thessaloniki
Carotid Atherosclerosis-Stroke-Type 2 Diabetes-Metabolic Syndrome
September 2005
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