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Rimonabant

Basic information Description References Safety Related Supplier
Rimonabant Basic information
Rimonabant Chemical Properties
Rimonabant Usage And Synthesis
  • DescriptionRimonabant is an inverse antagonist for the cannabinoid receptor (CB1). It acts by selectively blocking CB1 receptors found in the brain and in peripheral organs important in glucose and lipid metabolism, including adipose tissue, the liver, gastrointestinal tract, and muscle. Thus, rimonabant constitutes a therapeutic approach to obesity and cardiovascular risk factors. As an anorectic antiobesity drug, it was used as an adjunct to diet and exercise for obese or overweight patients with associated risk factors in Europe in 2006. Nevertheless, adverse effects including suicidality, depression, and anxiety were reported, based on which rimonadant was withdrawn worldwide in 2008.
    Andogenous cannabinoids are related to the pleasurable effect of nicotine, rimonabant, as a cannabinoid receptor blocker, is also being tested as a potential anti-smoking treatment.
  • References[1] https://www.drugs.com/acomplia.html
    [2] Leite CE, Mocelin CA, Petersen GO, Leal MB, Thiesen FV (2009) Rimonabant: an antagonist drug of the endocannabinoid system for the treatment of obesity, Pharmacol Rep., 61, 217-224
  • DescriptionRimonabant is a first-in-class drug launched as an oral treatment for obesity, and its mechanism of action involves the selective antagonism of cannabinoid type 1 (CB1) receptor. It is specifically indicated as an adjunct to diet and exercise for the treatment of obese patients (body mass index [BMI]≥30 kg/m2), or overweight patients (BMI>27 kg/m2) with associated risk factors such as type 2 diabetes or dyslipidemia. Additionally, rimonabant is currently under development as a treatment for nicotine dependence. The CB1 and CB2 receptors, along with their endogenous ligands, constitute the endocannabinoid system. The CB1 receptor is expressed in the brain, adipose tissue, and several peripheral organs; the CB2 receptor is predominantly expressed in immune cells. Activation of the CB1 receptor in the CNS is associated with appetite stimulation and the modulation of brain reward mechanism, whereas activation in the periphery favors metabolic processes that lead to hepatic lipogenesis and impaired glucose homeostasis. Rimonabant acts by selectively blocking the action of central and peripheral CB1 receptors, thereby reducing food intake and improving lipid and glucose metabolism.
  • OriginatorSanofi-Synthelabo (France)
  • UsesRimonabant is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane
  • brand nameAcomplia (Sanofi-Synthe-labo).
Rimonabant(168273-06-1)Related Product Information
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