Rimonabant 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.
Verwenden
Rimonabant is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane
Rimonabant Upstream-Materialien And Downstream Produkte
RimonabantQ: What is
Rimonabant Q: What is the CAS Number of
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Rimonabant
Rimonaban
Rimonabant in methanol
168273-06-1
C22Cl3HN4O
C22H21Cl3N4O
SR141716
Weight Loss
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