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Paroxetine hydrochloride

Catalog No. T1636   CAS 78246-49-8
Synonyms: Paroxetine HCl, BRL29060 hydrochloride, FG-7051, BRL29060A

Paroxetine hydrochloride (Paroxetine HCl) is a serotonin uptake inhibitor that is effective in the treatment of depression.

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Paroxetine hydrochloride Chemical Structure
Paroxetine hydrochloride, CAS 78246-49-8
Pack Size Availability Price/USD Quantity
25 mg In stock $ 45.00
50 mg In stock $ 54.00
100 mg In stock $ 78.00
200 mg In stock $ 112.00
500 mg In stock $ 153.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 99.91%
Purity: 99.61%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Paroxetine hydrochloride (Paroxetine HCl) is a serotonin uptake inhibitor that is effective in the treatment of depression.
Targets&IC50 GRK2:14 μM
In vitro Paroxetine, at an ED50 of 1-3 mg/kg when administered orally (PO), demonstrates the capability to prevent the depletion of serotonin (5-HT) in rats' brains induced by p-chloroamphetamine (PCA), signifying an inhibition of serotonin uptake in vivo. Additionally, in isolated rat hypothalamic synaptosomes, paroxetine exhibits a dose-dependent inhibition of [3H] - 5-HT uptake with an ED50 of 1.9 mg/kg, while showing minimal effects on the uptake of [3H] - norepinephrine (NA), with an ED50 exceeding 30 mg/kg.
In vivo Paroxetine, a highly effective hydroxylated metabolite inhibitor of (dextromethorphan), demonstrates the concentration-dependent reduction in the firing rate of serotonergic neurons within the DRN of super fused brainstem slices at 1-300 μM, with an IC50 value of 1.4 μM. With an inhibition constant (Ki) of 2 mM, Paroxetine's inhibitory capacity surpasses that of fluoxetine or norfluoxetine, indicating its more potent effect. Moreover, in rat cortical and in vitro hypothalamic synapses, Paroxetine acts as a potent and specific inhibitor of [3H]-5-hydroxytryptamine (5-HT), with a Ki of 1.1 nM. Its antidepressant activity is attributed to the increased concentration of 5-HT in the extracellular compartment, thereby enhancing serotonergic neurotransmission. Paroxetine also inactivates CYP2D6 by forming metabolic intermediate complexes.
Cell Research Paroxetine is dissolved in DMSO. Cell viability is determined by the tetrazolium salt 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) assay. BV2 and primary microglial cells are initially seeded into 96-well plates at a density of 1×104 cells/well and 5×104 cells/well, respectively. Following treatment, MTT (5 mg/mL in PBS) is added to each well and incubated at 37°C for four hours. The resulting formazan crystals are dissolved in dimethylsulfoxide (DMSO). The optical density is measured at 570 nm, and results are expressed as a percentage of surviving cells compared with the control.
Synonyms Paroxetine HCl, BRL29060 hydrochloride, FG-7051, BRL29060A
Molecular Weight 365.826
Formula C19H21ClFNO3
CAS No. 78246-49-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 10 mg/mL (27.33 mM)

Ethanol: 35 mg/mL (95.67 mM)

DMSO: 73 mg/mL (199.54 mM)

TargetMolReferences and Literature

1. Le Poul E, et al. Naunyn Schmiedebergs Arch Pharmacol, 1995, 352(2), 141-148. 2. von Moltke LL, et al. J Clin Psychopharmacol, 1995, 15(2), 125-131. 3. Thomas DR, et al. Psychopharmacology (Berl), 1987, 93(2), 193-200. 4. Bertelsen KM, et al. Drug Metab Dispos, 2003, 31(3), 289-293. 6. Lassen TR, et al. Effect of paroxetine on left ventricular remodeling in an in vivo rat model of myocardial infarction. Basic Res Cardiol. 2017 May;112(3):26. 7. Waldschmidt HV, et al. Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine. J Med Chem. 2017 Apr 13;60(7):3052-3069. 8. Wang K, Gong Q, Zhan Y, et al. Blockage of autophagic flux and induction of mitochondria fragmentation by Paroxetine hydrochloride in lung cancer cells promotes apoptosis via the ROS-MAPK pathway[J]. Frontiers in Cell and Developmental Biology. 2020, 7: 397.

TargetMolCitations

1. Wang K, Gong Q, Zhan Y, et al. Blockage of autophagic flux and induction of mitochondria fragmentation by Paroxetine hydrochloride in lung cancer cells promotes apoptosis via the ROS-MAPK pathway. Frontiers in Cell and Developmental Biology. 2020, 7: 397

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Membrane Protein-targeted Compound Library Kinase Inhibitor Library Anti-Neurodegenerative Disease Compound Library FDA-Approved Kinase Inhibitor Library GPCR Compound Library Inhibitor Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library

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Keywords

Paroxetine hydrochloride 78246-49-8 Autophagy GPCR/G Protein Neuroscience AChR GRK 5-HT Receptor Serotonin Transporter BRL 29060 Hydrochloride Paroxetine Hydrochloride BRL 29060 FG7051 Paroxetine HCl inhibit Paroxetine BRL29060 Hydrochloride SLC6A4 BRL-29060 Hydrochloride BRL29060 FG 7051 Inhibitor SERT BRL29060 hydrochloride BRL-29060 5-HTT FG-7051 BRL29060A inhibitor

 

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