Lofepramine-d3
Lofepramine-d3 (Lopramine-d3) is the deuterium labeled Lofepramine. Lofepramine (Lopramine) is a potent tricyclic antidepressant and is extensively metabolised to Desipramine. The antidepressant activity of Lofepramine stems from the facilitation of noradrenergic neurotransmission by uptake inhibition. Lofepramine may also potentiate serotoninergic neurotransmission by inhibition of the neuronal uptake of serotonin and the enzyme tryptophan pyrrolase. Lofepramine has significant anxiolytic efficacy in addition to its antidepressant properties.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1185083-78-6
- 分子式: C26H24D3ClN2O
- 分子量:421.98
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
体外実験
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
アプリケーション
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
化学情報
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CAS 番号 1185083-78-6
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非標識Cas 23047-25-8
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分子量 421.98
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分子式 C26H24D3ClN2O
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SMILES
C(CCN(CC(=O)C1=CC=C(Cl)C=C1)C([2H])([2H])[2H])N2C=3C(CCC=4C2=CC=CC4)=CC=CC3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Protocol for Tail Suspension Test (TST)
The Tail Suspension Test is a mouse behavioral assay in which an animal is suspended by the tail in an inescapable position, causing alternating escape-directed activity and immobility; the main readout is immobility time, and antidepressant-like treatments generally reduce immobility compared with vehicle controls. The assay detects behavioral response to acute inescapable stress rather than a molecular event; immobility is interpreted as passive stress-coping behavior, while reduced immobility is used as a predictive screen for antidepressant-like activity, with important limitations related to strain, locomotor activity, and tail-climbing behavior.
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Protocol for Forced Swim Test (FST)
The Forced Swim Test is a rodent behavioral assay in which a mouse or rat is placed in an inescapable cylinder of water, and the main readout is the time spent immobile versus active escape-related behaviors such as swimming or climbing. Reduced immobility after treatment has historically been interpreted as antidepressant-like activity, but the assay should be interpreted as a behavioral response to acute inescapable stress rather than a complete model of human depression.
純度とドキュメンテーション
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [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]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)