Home Neuronal Signaling Serotonin Transporter inhibitor Paroxetine HCl For research use only.

Paroxetine HCl

Synonyms: BRL-29060A, FG-7051

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

Paroxetine HCl Chemical Structure

Paroxetine HCl Chemical Structure

CAS No. 78246-49-8

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Paroxetine HCl Related Products

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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05730062 Not yet recruiting
Opioid Induced Respiratory Depression|Depressive Disorder|Anxiety Disorders
Leiden University Medical Center
 March 15 2023 Phase 1
NCT05637671 Recruiting
Vasomotor Symptoms
Cairo University
 February 10 2022 Phase 3

Chemical Information & Solubility

Molecular Weight 365.83 Formula

C19H20FNO3.HCl
CAS No. 78246-49-8 SDF Download Paroxetine HCl SDF
Smiles C1CNCC(C1C2=CC=C(C=C2)F)COC3=CC4=C(C=C3)OCO4.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 73 mg/mL ( (199.54 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 35 mg/mL

Water : 10 mg/mL


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In vivo
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