Paroxetine HCl

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

Paroxetine HCl Chemical Structure

Molecular Weight(MW): 365.83

Paroxetine HCl is an antidepressant drug of the SSRI type.

Size Price Stock Quantity  
In DMSO USD 90 In stock
USD 70 In stock
USD 210 In stock
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Biological Activity

Description Paroxetine HCl 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

Solubility (25°C)

In vitro DMSO 73 mg/mL (199.54 mM)
Ethanol 35 mg/mL (95.67 mM)
Water 1 mg/mL (2.73 mM)

* 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 powder
in solvent
Synonyms BRL-29060A, FG-7051

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03879746 Not yet recruiting Premature Ejaculation Assiut University April 2019 Phase 3
NCT03879746 Not yet recruiting Premature Ejaculation Assiut University April 2019 Phase 3
NCT03779789 Not yet recruiting Major Depressive Disorder Azienda Ospedaliera Universitaria Integrata Verona|University of Catania February 1 2019 Phase 4
NCT03779789 Not yet recruiting Major Depressive Disorder Azienda Ospedaliera Universitaria Integrata Verona|University of Catania February 1 2019 Phase 4
NCT03538691 Recruiting Major Depressive Disorder Otsuka Pharmaceutical Development & Commercialization Inc. July 13 2018 Phase 3
NCT03538691 Recruiting Major Depressive Disorder Otsuka Pharmaceutical Development & Commercialization Inc. July 13 2018 Phase 3

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