Paroxetine HCl

For research use only.

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

1 publication

Paroxetine HCl Chemical Structure

CAS No. 78246-49-8

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

Selleck's Paroxetine HCl has been cited by 1 publication

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Biological Activity

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


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


CAS No. 78246-49-8
Storage powder
in solvent
Synonyms BRL-29060A, FG-7051
Smiles C1CNCC(C1C2=CC=C(C=C2)F)COC3=CC4=C(C=C3)OCO4.Cl

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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
NCT02932904 Completed Drug: Vortioxetine|Drug: Paroxetine|Drug: Placebo Healthy Volunteers Takeda November 21 2016 Phase 4

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