Paroxetine-d4
Paroxetine-d4 (BRL29060-d4) 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.
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- CAS. Nr.: 923932-45-0
- Formel: C19H16D4FNO3
- Molecular Weight:333.39
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
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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.
Chemical Information
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CAS. Nr. 923932-45-0
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Unlabeled Cas 61869-08-7
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Molecular Weight 333.39
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Formel C19H16D4FNO3
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SMILES
[2H]C1([2H])OC2=CC=C(C=C2O1)OC([2H])([2H])[C@H]3[C@H](C4=CC=C(C=C4)F)CCNC3
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Synonyms
BRL29060-d4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Paroxetine-d4 Related Classifications
HY-122272S Related Classifications
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- Paroxetine-d4
- 923932-45-0
- BRL29060-d4
- 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