Paroxetine-d2
Paroxetine-d2 (BRL29060-d2) is the deuterated-labeled Paroxetine (HY-122272). Paroxetine (BRL29060) is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 923932-43-8
- 分子式: C19H18D2FNO3
- 分子量:331.38
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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CYP2D6 |
5-HT2 Receptor |
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Cell Line:Raw264.7 mouse macrophages
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Concentration:10 μM; 20 μM
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Incubation Time:6 h; 24 h
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Result:Reduced LPS-induced IL-6 production to ~75% of LPS-only levels at 6 hours with 10 μM.
Reduced LPS-induced IL-6 production to ~50% of LPS-only levels at 6 hours with 20 μM.
Reduced LPS-induced IL-6 production to ~80% of LPS-only levels at 24 hours with 10 μM.
Reduced LPS-induced IL-6 production to ~60% of LPS-only levels at 24 hours with 20 μM.
Increased LPS-induced TNFα production to ~155% of LPS-only levels at 6 hours with 10 μM.
Increased LPS-induced TNFα production to ~195% of LPS-only levels at 6 hours with 20 μM.
Increased LPS-induced TNFα production to ~120% of LPS-only levels at 24 hours with 10 μM.
Increased LPS-induced TNFα production to ~145% of LPS-only levels at 24 hours with 20 μM.
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Cell Line:Raw264.7 mouse macrophages pretreated with 5-HT2/5-HT7 receptor antagonist LY215840
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Concentration:20 μM
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Incubation Time:24 h
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Result:Reduced LPS-induced IL-6 production to ~45% of LPS-only levels.
Increased LPS-induced TNFα production to ~180% of LPS-only levels.
Co-treatment with LY215840 (10 nM, 100 nM, 1 μM) further reduced IL-6 levels to below ~20% of LPS-only levels.
Co-treatment with LY215840 (10 nM, 100 nM, 1 μM) reversed TNFα enhancement, reducing levels to ~80%, ~40%, and ~40% of LPS-only levels, respectively (for 100 nM and 1 μM LY215840).
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Animal Model:Male Sprague-Dawley rats[6]
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Dosage:0.3, 1, 3, 10 mg/kg; single dose
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Administration:p.o.
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Result:Reduced the synthesis rate of serotonin and increased the social time of rats, but had no effect on motor activity. The motor activity of animals taking the drug for a long time was slightly lower than that of animals taking the drug for a short time.
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 923932-43-8
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非標識Cas 61869-08-7
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分子量 331.38
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分子式 C19H18D2FNO3
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SMILES
FC1=CC=C([C@H]2[C@H](COC3=CC=C(OC([2H])([2H])O4)C4=C3)CNCC2)C=C1
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別名
BRL29060-d2
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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.
純度とドキュメンテーション
参考文献
[1]. Bourin M, et al. Paroxetine: a review[J]. CNS drug reviews, 2001, 7(1): 25-47.
[2]. Nevels RM, et al. Paroxetine-The Antidepressant from Hell? Probably Not, But Caution Required. Psychopharmacology bulletin. 2016 Mar 01;46(1):77-104. [Content Brief]
[3]. Durairaj H, et al. Paroxetine differentially modulates LPS-induced TNFα and IL-6 production in mouse macrophages. International immunopharmacology. 2015 Apr;25(2):485-92. [Content Brief]
[4]. Young-Woo Cho, et al. Paroxetine Induces Apoptosis of Human Breast Cancer MCF-7 Cells through Ca2+-and p38 MAP Kinase-Dependent ROS Generation. Cancers (Basel). 2019 Jan 9;11(1):64. [Content Brief]
[5]. Malek Zarei, et al. Paroxetine attenuates the development and existing pain in a rat model of neurophatic pain. Iran Biomed J. 2014;18(2):94-100. [Content Brief]
[6]. S Lightowler, et al. Anxiolytic-like effect of paroxetine in a rat social interaction test. Pharmacol Biochem Behav. 1994 Oct;49(2):281-5. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Paroxetine-d2 関連分類
HY-111124 関連分類
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- Paroxetine-d2
- 923932-43-8
- BRL29060-d2
- Isotope-Labeled Compounds
- Cytochrome P450
- 5-HT Receptor
- NO Synthase
- Apoptosis
- Serotonin Transporter
- Estrogen Receptor/ERR
- 5-HT2 receptors
- Raw264.7 mouse macrophages
- nitric oxide synthase
- 5-HT1B/1D autoreceptors
- serotonin reuptake transporter
- cytochrome P450 3A4
- 5-HT1A autoreceptor
- norepinephrine reuptake transporter
- cytochrome P450 2D6
- muscarinic cholinergic receptor
- Inhibitor
- inhibitor
- inhibit