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Technical Data
| Formula | C19H20FNO3.HCl |
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| Molecular Weight | 365.83 | CAS No. | 78246-49-8 | |
| 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) | |||
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* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | Paroxetine HCl (BRL-29060A, FG-7051) is an antidepressant drug of the SSRI type. | ||
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| Targets |
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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. [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)
References
Selleck's Paroxetine HCl has been cited by 4 publications
| Neddylation inhibition induces glutamine uptake and metabolism by targeting CRL3SPOP E3 ligase in cancer cells [ Nat Commun, 2022, 13(1):3034] | PubMed: 35641493 |
| DNA repair proteins as the targets for paroxetine to induce cytotoxicity in gastric cancer cell AGS [ Am J Cancer Res, 2022, 12(4):1465-1483] | PubMed: 35530295 |
| Utilizing an Endogenous Progesterone Receptor Reporter Gene for Drug Screening and Mechanistic Study in Endometrial Cancer [ Cancers (Basel), 2022, 14(19)4883] | PubMed: 36230806 |
| A multi-residue analytical method for extraction and analysis of pharmaceuticals and other selected emerging contaminants in sewage sludge [ Anal Methods, 2021, 10.1039/d0ay02027c] | PubMed: 33447838 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.