Clomipramine (Chlorimipramine) hydrochloride 有效阻断 5-HT 再摄取 (5-HT reuptake),IC50值为 1.5 nM。Clomipramine 是一种三环类抗抑郁药,可用于抑郁症和强迫症(OCD)的研究。
生物活性 | Clomipramine (Chlorimipramine) hydrochloride is a potent5-HT reuptakeblocker with theIC50value of 1.5 nM. Clomipramine hydrochloride is a tricyclic antidepressant that can be used for the research of depression and obsessive compulsive disorder (OCD)[1]. |
体外研究 (In Vitro) | Clomipramine hydrochloride can inhibit reuptake of both noradrenaline and 5-HT, although Clomipramine inhibits 5-HT reuptake more strongly than it inhibits noradrenaline reuptake[1]. The antidepressant Clomipramine inhibits both venom AChE as well as human serum BChE in a concentration-dependent manner but has no effect on AChE in the rat brain striatum[2].
Clomipramine hydrochloride interferes with the autophagic flux and severely compromises the viability of tumorigenic cells upon cytotoxic stress[3]. Clomipramine hydrochloride reduces autophagy in neuronal primary cultures. Clomipramine (1 and 5 μM) hydrochloride negatively regulates neuronal autophagic pathway in primary cultured cells[3].
Western Blot Analysis[3] Cell Line: | Primary cortical neurons | Concentration: | 1 and 5 μM | Incubation Time: | 12, 24 and 48 hours | Result: | Enhanced the LC3-I conversion to LC3-II in a concentration-dependent manner at all analyzed time points. |
|
体内研究 (In Vivo) | Clomipramine (5-20 mg/kg; i.p) hydrochloride elicits significant hyperglycemia in mice. Clomipramine hydrochloride induces hyperglycemia in mice by blocking the 5-HT2B and/or 5-HT2C receptors, which results in facilitation of adrenaline release. In mice, Clomipramine hydrochloride reduces immobility in the forced swimming test, which is the behavioral model for antidepressants. Clomipramine hydrochloride also inhibits the OCD animal model, marble burying behavior in mice[1].
Clomipramine (20 mg/kg) hydrochloride decreases autophagic flux in murine tissues[3].
Animal Model: | C57BL/6 J mice (6 weeks of age and 22 to 25 g)[3] | Dosage: | 20 mg/kg | Administration: | Treated intraperitoneally for 21 days | Result: | Both LC3-II and p62 were significantly increased in the liver of Clomipramine treated mice compared to vehicle treated ones. |
|
Clinical Trial | |
分子量 | |
性状 | |
Formula | |
CAS 号 | |
中文名称 | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: H2O : ≥ 50 mg/mL(142.32 mM) DMSO : 50 mg/mL(142.32 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 2.8465 mL | 14.2324 mL | 28.4649 mL | 5 mM | 0.5693 mL | 2.8465 mL | 5.6930 mL | 10 mM | 0.2846 mL | 1.4232 mL | 2.8465 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: PBS Solubility: 100 mg/mL (284.65 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 3 mg/mL (8.54 mM); Clear solution
此方案可获得 ≥ 3 mg/mL (8.54 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 3 mg/mL (8.54 mM); Clear solution
此方案可获得 ≥ 3 mg/mL (8.54 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 4. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 3 mg/mL (8.54 mM); Clear solution
此方案可获得 ≥ 3 mg/mL (8.54 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
|