Paroxetine hydrochloride

SKU: orb1307940

Description

Paroxetine hydrochloride is a selective serotonin reuptake inhibitor (SSRI) used in depression research. It is widely applied in both in vitro binding assays and in vivo behavioral studies to investigate serotonergic neurotransmission and antidepressant mechanisms.

Research Area

Cell Biology, Neuroscience, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	78246-49-8
MW	365.826
Purity	99.99%
Formula	C₁₉H₂₁ClFNO₃
SMILES	Cl.Fc1ccc(cc1)[C@@H]1CCNC[C@H]1COc1ccc2OCOc2c1
Target	AChR,Autophagy,GRK,5-HT Receptor,Serotonin Transporter
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.47 mM);Ethanol:35 mg/mL (95.67 mM);H2O:10 mg/mL (27.34 mM);DMSO:45 mg/mL (123.01 mM)

Bioactivity

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Target IC50	GRK2:14 μM
In Vivo	Paroxetine, a highly effective hydroxylated metabolite inhibitor of (dextromethorphan), demonstrates the concentration-dependent reduction in the firing rate of serotonergic neurons within the DRN of super fused brainstem slices at 1-300 μM, with an IC50 value of 1.4 μM. With an inhibition constant (Ki) of 2 mM, Paroxetine's inhibitory capacity surpasses that of fluoxetine or norfluoxetine, indicating its more potent effect. Moreover, in rat cortical and in vitro hypothalamic synapses, Paroxetine acts as a potent and specific inhibitor of [3H]-5-hydroxytryptamine (5-HT), with a Ki of 1.1 nM. Its antidepressant activity is attributed to the increased concentration of 5-HT in the extracellular compartment, thereby enhancing serotonergic neurotransmission. Paroxetine also inactivates CYP2D6 by forming metabolic intermediate complexes. Read more...
In Vitro	Paroxetine, at an ED50 of 1-3 mg/kg when administered orally (PO), demonstrates the capability to prevent the depletion of serotonin (5-HT) in rats' brains induced by p-chloroamphetamine (PCA), signifying an inhibition of serotonin uptake in vivo. Additionally, in isolated rat hypothalamic synaptosomes, paroxetine exhibits a dose-dependent inhibition of [3H] - 5-HT uptake with an ED50 of 1.9 mg/kg, while showing minimal effects on the uptake of [3H] - norepinephrine (NA), with an ED50 exceeding 30 mg/kg. Read more...
Cell Research	Paroxetine is dissolved in DMSO. Cell viability is determined by the tetrazolium salt 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) assay. BV2 and primary microglial cells are initially seeded into 96-well plates at a density of 1×104 cells/well and 5×104 cells/well, respectively. Following treatment, MTT (5 mg/mL in PBS) is added to each well and incubated at 37°C for four hours. The resulting formazan crystals are dissolved in dimethylsulfoxide (DMSO). The optical density is measured at 570 nm, and results are expressed as a percentage of surviving cells compared with the control. Read more...

Storage & Handling

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Storage	keep away from moisture \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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BRL 29060, BRL 29060 Hydrochloride, BRL29060, BRL-29060, BRL29060 Hydrochloride, BRL29060 hydrochloride, BRL-29060 Hydrochloride, BRL29060A, Autophagy, 5HTReceptor, 5HT Receptor, 5-HT, 5-HTT, AChR, Paroxetine, Paroxetine HCl, Paroxetine Hydrochloride, Paroxetine hydrochloride, inhibit, Inhibitor, FG 7051, FG7051, FG-7051, GRK2, SLC6A4, Serotonin Transporter, SerotoninTransporter, SERT

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Compound Identifiers

PubChem CID

62878 ↗

Key Properties

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No computed properties available.

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