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Rimonabant

CAS No. : 168273-06-1

MCE 站：Rimonabant

产品活性：Rimonabant (SR141716) 是中心大麻素受体 1 (CB1) 高效的、选择性的、能透过血脑屏障的拮抗剂， K_i 值为 1.8 nM。Rimonabant (SR141716) 也能够抑制分枝杆菌膜蛋白3 (MMPL3)。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Anti-infection

作用靶点：Cannabinoid Receptor  |  Bacterial

In Vitro: Rimonabant could inhibit the growth of Mtb with an MIC of 54 μM. MmpL3, an anti-TB target, is the direct target of rimonabant.
Rimonabant itself (10^-12-10^-3 M, 12 concentrations) inhibits the basal binding of [³⁵S]GTPgS to human cortical membranes in a concentration dependent manner, with a -log IC₅₀ of 4.7±0.2 (IC₅₀ = 20 μM) and a maximal inhibition of 48±2%.

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 and MCP-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 .
Rimonabant (20 mg daily) exhibits a significant reduction in many cardiometabolic risk factors.

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