Paroxetine HCl

Catalog No.S3005 Synonyms: BRL-29060A, FG-7051

For research use only.

Paroxetine HCl (BRL-29060A, FG-7051) is an antidepressant drug of the SSRI type.

Paroxetine HCl Chemical Structure

CAS No. 78246-49-8

Selleck's Paroxetine HCl has been cited by 1 Publication

Purity & Quality Control

Choose Selective Serotonin Transporter Inhibitors

Biological Activity

Description Paroxetine HCl (BRL-29060A, FG-7051) is an antidepressant drug of the SSRI type.
Targets
AChR [1] 5-HT [1]
In vitro

Paroxetine apparently exerts their antidepressant activity by increasing the concentration of 5-HT in the extracellular compartment, thereby enhancing serotoninergic neurotransmission. Paroxetine (1-300 μM) results in a concentration-dependent reduction in the firing rate of DRN serotoninergic neurons with IC50 values of 1.4 μM in the ACSF superfusing brain stem slices. [1] Paroxetine is a highly potent inhibitor of desipramine hydroxylation, the inhibition constant (Ki) value of 2.0 mM indicated greater inhibiting potency than fluoxetine or norfluoxetine. [2] Paroxetine is shown to be a potent (Ki = 1.1 nM) and specific inhibitor of [3H]-5-hydroxytryptamine (5-HT) uptake into rat cortical and hypothalamic synaptosomes in vitro. Paroxetine demonstrates weak affinity for muscarinic receptors (Ki = 89 nM) but is at least 15 fold weaker than amitriptyline (Ki = 5.1 nM). [3] Paroxetine inactivates CYP2D6 via the formation of a metabolite intermediate complex. [4]

In vivo Paroxetine produces a dose-related inhibition of [3H]-5-HT uptake (ED50 = 1.9 mg/kg) into rat hypothalamic synaptosomes ex vivo with little effect on [3H]-l-noradrenaline (NA) uptake (ED50 greater than 30 mg/kg). Paroxetine (ED50 1-3 mg/kg PO) prevents the 5-HT depleting effect of p-chloroamphetamine (PCA) in rat brain, demonstrating 5-HT uptake blockade in vivo. [3]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 73 mg/mL
(199.54 mM)
Water 1 mg/mL
(2.73 mM)
Ethanol ''' 35 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 365.83
Formula

C19H20FNO3.HCl

CAS No. 78246-49-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CNCC(C1C2=CC=C(C=C2)F)COC3=CC4=C(C=C3)OCO4.Cl

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03329573 Completed Drug: Paroxetine IR tablets A|Drug: Paroxetine IR tablets B Anxiety Disorders GlaxoSmithKline May 30 2018 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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