research use only
Cat.No.S3005
| Related Targets | Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) |
|---|---|
| Other Serotonin Transporter Inhibitors | Dapoxetine |
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In vitro |
DMSO
: 73 mg/mL
(199.54 mM)
Ethanol : 35 mg/mL Water : 1 mg/mL |
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In vivo |
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| Molecular Weight | 365.83 | Formula | C19H20FNO3.HCl |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 78246-49-8 | Download SDF | Storage of Stock Solutions |
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| Synonyms | BRL-29060A, FG-7051 | SMILES | C1CNCC(C1C2=CC=C(C=C2)F)COC3=CC4=C(C=C3)OCO4.Cl | ||
Read more about storage stability stock solution CAS number SMILES
| Targets/IC50/Ki |
AChR
5-HT
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|---|---|
| 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. 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. 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). Paroxetine inactivates CYP2D6 via the formation of a metabolite intermediate complex.
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| 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.
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References |
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(data from https://clinicaltrials.gov, updated on 2026-09-02)
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|---|---|---|---|---|---|
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| NCT07318181 | RECRUITING | Post Traumatic Stress Disorder; Post Traumatic Stress Disorder PTSD; Post-Traumatic Stress Disorder, PTSD |
University of Luxembourg |
2026-01-01 | |
| NCT07715669 | RECRUITING | Preeclampsia; Endothelial Function |
Anna Stanhewicz, PhD |
2026-08-30 | EARLY_PHASE1 |
| NCT07025590 | RECRUITING | Cardiovascular Diseases (CVD); Depression Anxiety Disorder |
Guangdong Provincial People's Hospital |
2025-04-22 | |
| NCT06796946 | NOT_YET_RECRUITING | Deprescription; Antidepressants |
University of Huelva |
2026-06 | EARLY_PHASE1 |
| NCT06799169 | ACTIVE_NOT_RECRUITING | Tinnitus |
University of California, Irvine |
2025-06-01 | PHASE4 |
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