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Sibutramine hydrochloride

CAS No. : 84485-00-7

MCE 站：Sibutramine hydrochloride

产品活性：Sibutramine hydrochloride 是一种新型的 5-HT (serotonin) 和去甲肾上腺素再摄取抑制剂 (SNRI)。Sibutramine 抑制电压门控 K⁺ 通道 K_V4.3，IC₅₀ 为 17.3 μM。

研究领域：Neuronal Signaling  |  Membrane Transporter/Ion Channel

作用靶点：Serotonin Transporter  |  Potassium Channel

In Vitro: Sibutramine is a novel 5-HT (serotonin) ａnd noradrenaline reuptake inhibitor (SNRI). Sibutramine reduces the food intake of rodents ａnd this effect is partially or completely reversed by pretreating with 5-HT or noradrenaline antagonists, indicating that both neurotransmitters are involved in sibutramine＇s hypophagic effect. Sibutramine causes the concentration-dependent block of the K_V1.3 ａnd K_V3.1 currents with IC₅₀s of 3.7 ａnd 32.7 μM, respectively. The steady-state currents of K_V1.3 ａnd K_V3.1 are decreased by Sibutramine in a concentration-dependent manner with IC₅₀s of 3.7±0.7 (n=6) ａnd 32.7±5.0 μM (n=5), respectively.

In Vivo: Sibutramine (SIB) (5 mg/kg ip), which blocks the reuptake of both 5-hydroxytryptamine (5-HT) ａnd noradrenaline (NA), also requires ARC pro-opiomelanocortin (POMC) neurons to achieve its appetitive effects in male ａnd female mice. Sibutramine (5 mg/kg) suppresses 3-hour dark cycle food intake to a comparable extent in young adult ａnd middle-aged male ａnd female POMC-EGFP mice. In normal Wistar rats, 3 mg/kg Sibutramine produces a marked (~30%) inhibition of food intake on the first day of dosing. Consistent with published data, the effects of Sibutramine on food intake diminished with time, although cumulative food intake over the 9-day study is significantly (P<0.001) lower in Sibutramine-treated (213.3±5.7 g) than in vehicle-treated (260.2±3.0 g) rats. Sibutramine also significantly reduces overall body weight gain (vehicle 30±2 g, Sibutramine 14±3 g; P<0.001).

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