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。

Sibutramine hydrochloride is a novel 5-HT (serotonin) and noradrenaline reuptake inhibitor (SNRI). The IC 50 for Sibutramine block of voltage-gated K channel (K V )4.3 is 17.3 μM.

Solid

5-HT (serotonin) reuptake
IC50: 17.3 μM (KV4.3)

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 sibutramines hypophagic effect. Sibutramine causes the concentration-dependent block of the KV1.3 and KV3.1 currents with IC50s of 3.7 and 32.7 μM, respectively. The steady-state currents of KV1.3 and KV3.1 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. has not independently confirmed the accuracy of these methods. They are for reference only.

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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[1]. Heal DJ, et al. Sibutramine: a novel anti-obesity drug. A review of the pharmacological evidence to differentiate it from d-amphetamine and d-fenfluramine. Int J Obes Relat Metab Disord. 1998 Aug;22 Suppl 1:S18-28; discussion S29.
[2]. Kim SE, et al. Open channel block of A-type, k_v4.3, and delayed rectifier K channels, K_V1.3 and K_V3.1, bySibutramine. J Pharmacol Exp Ther. 2007 May;321(2):753-62.

In Vitro: DMSO : ≥ 57 mg/mL (180.20 mM)配制储备液