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    Paroxetine HCl (BRL29060)
    Paroxetine HCl (BRL29060)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1164
    CAS #: 78246-49-8Purity ≥98%

    Description: Paroxetine HCl (formerly BRL-29060A, BRL29060A, FG7051; FG-7051), the hydrochloride salt of Paroxetine, is a potent and selective serotonin uptake inhibitor (SSRI) that is effective in the treatment of depression. It is commonly prescribed as an antidepressant and has GRK2 inhibitory ability with IC50 of 14 μM .Paroxetine binds to the pre-synaptic serotonin transporter complex resulting in negative allosteric modulation of the complex thereby blocking reuptake of serotonin by the pre-synaptic transporter. Paroxetine HCl has also displayed a high affinity for muscarinic acetylcholine receptors.

    References: Naunyn Schmiedebergs Arch Pharmacol. 1995 Aug;352(2):141-8; Psychopharmacology (Berl). 1987;93(2):193-200.

    Related CAS#: 61869-08-7 (Paroxetine); 64006-44-6 (Paroxetine maleate); 217797-14-3 (Paroxetine Mesylate) 78246-49-8 (HCl)   72471-80-8 (acetate) 110429-36-2 (N-methyl Paroxetine)

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    Molecular Weight (MW)365.83
    FormulaC19H20FNO3.HCl 
    CAS No.78246-49-8  (HCl);
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 73 mg/mL (199.5 mM)
    Water: 10 mg/mL (27.3 mM)
    Ethanol: 35 mg/mL (95.7 mM)
    Other infoChemical Name: (3S,4R)-3-((benzo[d][1,3]dioxol-5-yloxy)methyl)-4-(4-fluorophenyl)piperidine hydrochloride
    InChi Key: GELRVIPPMNMYGS-RVXRQPKJSA-N
    InChi Code: InChI=1S/C19H20FNO3.ClH/c20-15-3-1-13(2-4-15)17-7-8-21-10-14(17)11-22-16-5-6-18-19(9-16)24-12-23-18;/h1-6,9,14,17,21H,7-8,10-12H2;1H/t14-,17-;/m0./s1
    SMILES Code: FC1=CC=C([[email protected]]2[[email protected]](COC3=CC=C(OCO4)C4=C3)CNCC2)C=C1.[H]Cl
    SynonymsBRL-29060A, BRL29060A, FG7051; FG 7051; Paroxetine HCl; Paroxetine Hydrochloride; BRL 29060A, FG-7051; BRL29060 hydrochloride; BRL29060A; BRL 29060; BRL-29060


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    In Vitro

    In vitro activity: 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.


    Cell Assay: 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.

    In VivoParoxetine 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. 
    Animal modelRats
    Formulation & DosageAnimals are divided into two main groups: 1) pre-emptive and 2) post-injury group. Each main group is divided into three different subgroups: I) CCI vehicle-treated group, II) sham group, and III) CCI paroxetine-treated group. Vehicle is injected i.p. to CCI and sham-operated animals. In the pre-emptive study, paroxetine (10 mg/kg) is injected 1 h before surgery and continued daily until day 14 post surgery. In the post-injury group, paroxetine (10 mg/kg) is administered at day 7 post injury and continued daily until day 14. All behavioral tests are recorded on day 0 (control day) before surgery and on days 1, 3, 5, 7, 10, and 14 post-nerve injury.
    ReferencesNaunyn Schmiedebergs Arch Pharmacol. 1995 Aug;352(2):141-8; Psychopharmacology (Berl). 1987;93(2):193-200.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Paroxetine HCl

    Potencies of SERT homologues & mutants for paroxetine, as assessed by (a–g) inhibition of 20 nM [3H]5-HT transport in transiently-transfected T-REx-293 cells or (h) inhibition of 0.2 nM [125I]RTI-55 binding to crude membranes prepared from transiently-transfected T-REx-293 cells. Sci Rep. 2016; 6: 23789.
     

    Paroxetine HCl

    (A) Paroxetine metabolism (5 μmol/L) in hepatic microsomes of rats and (B) corresponding paroxetine clearance parameters in hepatic microsomes (Clapp, h).
     

    Paroxetine HCl

    Structure of LeuBAT complexed with paroxetine. Sci Rep. 2016; 6: 23789.


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