2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor 5-HT Receptor
  4. Lofepramine hydrochloride

Lofepramine hydrochloride  (Synonyms: Lopramine hydrochloride)

目录号: HY-12390A
产品使用指南 技术支持

Lofepramine (Lopramine) 是一种改良的三环类抗抑郁剂，口服有效。Lofepramine 抑制 Noradrenaline (NA) (HY-13715) 和 5-hydroxytryptamine (5-HT) 的摄取，其IC50s 值分别为 2.7 μM 和 11 μM。Lofepramine 通过促进去甲肾上腺素激活的神经传递发挥其抗抑郁活性。Lofepramine 还可以通过抑制神经元摄取 5-羟色胺和色氨酸吡咯酶来增强 5-羟色胺能神经传递。Lofepramine 还表现出显著的抗焦虑特性。

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Lofepramine hydrochloride Chemical Structure

Lofepramine hydrochloride Chemical Structure

CAS No. : 26786-32-3

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Lofepramine hydrochloride 的其他形式现货产品:

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Other Forms of Lofepramine hydrochloride:

Lofepramine hydrochloride 相关抗体

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α adrenergic receptor β adrenergic receptor

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Lofepramine (Lopramine) is a modified tricyclic and orally active antidepressant. Lofepramine inhibits the uptake of Noradrenaline (NA) (HY-13715) and 5-hydroxytryptamine (5-HT) with IC50s of 2.7 μM and 11 μM, respectively. Lofepramine exerts its antidepressant activity by promoting noradrenergic neurotransmission. Lofepramine also enhances serotonergic neurotransmission by inhibiting neuronal uptake of 5-HT and tryptophan pyrrolase. Lofepramine exhibits significant anxiolytic properties. [1][2][3][4].

体外研究
(In Vitro)

Lofepramine (0.01-100 μM, 10 min) 抑制小鼠脑细胞内3H-5-HT 和3H-NA 在突触体部分的摄取[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Lofepramine hydrochloride 相关抗体:
体内研究
(In Vivo)

Lofepramine (28-45 mg/kg, i.p., 实验前 1 h) 仅降低了用 SKF 525A 预处理的 28 mg/kg大鼠对这两种药物的摄取，并降低了 45 mg/kg 健康大鼠 对 5-HT 和 Noradrenaline (HY-13715) 的摄取[1]。
Lofepramine (50 mg /kg, i.p., 前 30 min 在脑室内给予 3H-5-HT (0.75μCi) 或3H-NA (1.2 μCi) 可有效抑制Noradrenaline (HY-13715) 摄取到两个组分 (P2- 和 S-组分) 中[1]。
Lofepramine (20 mg /kg, i.p., 每日一次, 连续 2 周) 及其去甲基代谢物 DMI (Desipramine) (HY-B1272A)，DML (Desmethyl Lofepramine) 和 DDMI (Desmethyl Desipramin) 在 OB (嗅球切除) 模型中表现出抗抑郁活性[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar strain rats, 150-200 g[1].
Dosage: 28, 45 mg/kg
Administration: i.p., 1 h before experiment , SKF 525A, 30 mg/kg, i.p., was injected 30 min before experiment.
Result: Did not influence the in vitro uptake of either 5-HT or noradrenaline in normal rats, but significantly decreased the uptake of both in rats at 28 mg/kg pretreated with SKF 525A.
Decreased significantly both 5-HT and noradrenaline uptake in intact rats at 45 mg/kg.
Animal Model: Male Wistar strain rats, 150-200 g[1].
Dosage: 30, 50 mg/kg
Administration: i.p., was injected 30 min before intraventricular administration of 3H-5-HT (0.75 μCi) or 3H-NA (1.2 μCi).
Result: Was also effective in inhibiting noradrenaline uptake into both fractions (the P2- and S-fractions) at 50 mg/kg.
Animal Model: Male Sprague-Dawley, 250–280 g. Bilateral olfactory bulbectomy (OB) was performed under anaesthesia (2.5% w/v; 10 mL/kg, i.p.)[4].
Dosage: 20 mg/kg
Administration: i.p., daily, 2 weeks
Result: Had no effects on immobility time.
Attenuated the increase in activity in the OB control group.
分子量

455.42

Formula

C26H28Cl2N2O
CAS 号
中文名称

盐酸洛非帕明
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Lofepramine hydrochloride 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lofepramine26786-32-3Lopramine盐酸洛非帕明Adrenergic Receptor5-HT ReceptorBeta ReceptorSerotonin Receptor5-hydroxytryptamine Receptorantidepressantsanxiolyticsleep EEGREM sleepInhibitorinhibitorinhibit

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