Lofepramine
Based on 1 Customer Validation
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. .
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- Reinheit: 99.36%
- CAS. Nr.: 23047-25-8
- Formel: C26H27ClN2O
- Molecular Weight:418.96
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Lofepramine (0.01-100 μM, 10 min) inhibits both 3H-5-HT and 3H-NA uptake into synaptosomal fractions in rats brain cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Lofepramine (50 mg /kg, i.p., was injected 30 min before intraventricular administration of 3H-5-HT (0.75 μCi) or 3H-NA (1.2 μCi)) is effective in inhibiting Noradrenaline (HY-13715) uptake into both fractions (the P2- and S-fractions) [1].
Lofepramine (20 mg /kg, i.p., daily, 2 weeks) and it’s desmethylated metabolites, DMI (Desipramine) (HY-B1272A), DML(Desmethyl lofepramine) and DDMI (Desmethyl desipramin), exhibits antidepressant activity in the OB (olfactory bulbectomy) model[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar strain rats, 150-200 g[1].
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Dosage:28, 45 mg/kg
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Administration:i.p., 1 h before experiment , SKF 525A, 30 mg/kg, i.p., was injected 30 min before experiment.
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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.
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Animal Model:Male Wistar strain rats, 150-200 g[1].
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Dosage:30, 50 mg/kg
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Administration:i.p., was injected 30 min before intraventricular administration of 3H-5-HT (0.75 μCi) or 3H-NA (1.2 μCi).
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Result:Was also effective in inhibiting noradrenaline uptake into both fractions (the P2- and S-fractions) at 50 mg/kg.
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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].
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Dosage:20 mg/kg
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Administration:i.p., daily, 2 weeks
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Result:Had no effects on immobility time.
Attenuated the increase in activity in the OB control group.
Chemical Information
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CAS. Nr. 23047-25-8
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Appearance Solid
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Molecular Weight 418.96
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Formel C26H27ClN2O
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Color White to yellow
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SMILES
CN(CC(C1=CC=C(Cl)C=C1)=O)CCCN2C3=CC=CC=C3CCC4=CC=CC=C42
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Synonyms
Lopramine
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (119.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (4.96 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Segawa T, et al. Effect of lofepramine and other antidepressants on the uptake of 5-hydroxytryptamine and noradrenaline into rat brain monoaminergic neurons. J Pharm Pharmacol. 1977 Mar;29(3):139-42. [Content Brief]
[2]. Lancaster SG, et al. Lofepramine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in depressive illness. Drugs. 1989 Feb;37(2):123-40. [Content Brief]
[3]. McIntyre RS, et al. The neurogenic compound, NSI-189 phosphate: a novel multi-domain treatment capable of pro-cognitive and antidepressant effects. Expert Opin Investig Drugs. 2017 Jun;26(6):767-770. [Content Brief]
[4]. Kelly JP, et al. An investigation of the antidepressant properties of lofepramine and its desmethylated metabolites in the forced swim and olfactory bulbectomized rat models of depression. Eur Neuropsychopharmacol. 1999 Jan;9(1-2):101-5. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3869 mL | 11.9343 mL | 23.8686 mL | 59.6716 mL |
| 5 mM | 0.4774 mL | 2.3869 mL | 4.7737 mL | 11.9343 mL | |
| 10 mM | 0.2387 mL | 1.1934 mL | 2.3869 mL | 5.9672 mL | |
| 15 mM | 0.1591 mL | 0.7956 mL | 1.5912 mL | 3.9781 mL | |
| 20 mM | 0.1193 mL | 0.5967 mL | 1.1934 mL | 2.9836 mL | |
| 25 mM | 0.0955 mL | 0.4774 mL | 0.9547 mL | 2.3869 mL | |
| 30 mM | 0.0796 mL | 0.3978 mL | 0.7956 mL | 1.9891 mL | |
| 40 mM | 0.0597 mL | 0.2984 mL | 0.5967 mL | 1.4918 mL | |
| 50 mM | 0.0477 mL | 0.2387 mL | 0.4774 mL | 1.1934 mL | |
| 60 mM | 0.0398 mL | 0.1989 mL | 0.3978 mL | 0.9945 mL | |
| 80 mM | 0.0298 mL | 0.1492 mL | 0.2984 mL | 0.7459 mL | |
| 100 mM | 0.0239 mL | 0.1193 mL | 0.2387 mL | 0.5967 mL |
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