"目录号: HY-14137
Rimonabant hydrochloride 是一种大麻素受体 (cannabinoid receptor) 拮抗剂，高亲和力地选择性结合到中枢大麻素受体 (CB1)，Ki为 2 nM。
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生物活性
Description
Rimonabant hydrochloride is acannabinoid receptorantagonist, which binds selectively to central cannabinoid receptors (CB1) with high affinity (Ki=2 nM).
IC50& Target
Ki: 2 nM (CB1 receptor)[1]
In Vitro
Rimonabant hydrochloride (SR 141716A) binds selectively to central cannabinoid receptors (CB1) with high affinity (Ki=2 nM), and blocks the inhibitory effects of cannabinoid receptor agonists in the mouse vas deferens, dopamine-stimulated adenylyl cyclase and WIN 55212-stimulated GTPγS binding[1]. Rimonabant dose-dependently inhibited CO synthesis in Raw 264.7 macrophages, with 1 μM producing a significant (~40%) decrease compared to untreated controls and concentrations ≥ 5 μM producing near complete inhibition. A small, but significant, reduction of TG and DG synthesis is also observed with Rimonabant at concentrations ≥ 10 μM. Inhibition of CO synthesis in Raw 264.7 macrophages by Rimonabant (IC50value 2.9±0.38 μM) is very similar to that of AM251 and SR144528 (IC50value 2.6±0.26 μM and 2.5±0.32 μM, respectively), two related compounds previously demonstrated to be potent ACAT inhibitors. Mouse peritoneal macrophages also displayed significantly reduced CO synthesis in response to Rimonabant treatment. Rimonabant at concentrations ≥ 1 μM significantly inhibits CO synthesis in CHO-ACAT1 and CHO-ACAT2 cells in a concentration-dependent manner with similar efficiency (IC50s of 1.5±1.2 μM and 2.2±1.1 μM, respectively)[2].
In Vivo
Pretreatment with Rimonabant hydrochloride (SR 141716A) blocks the antinociceptive, discriminative stimulus, memory impairing and hypolocomotor effects produced by Δ-9-THC. SR 141716A also precipitates a withdrawal syndrome in rats treated chronically with Δ-9-THC[1]. Pretreatment of mice with 0.1?mg/kg of WIN 55212-2 is effective in increasing the CPP induced by MDMA , while 1?mg/kg of Rimonabant specifically blocks CB1 receptors and does not act as an inverse agonist[3].
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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References
