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    Sertraline HCl
    Sertraline HCl

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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 #: V1029
    CAS #: 79559-97-0Purity ≥98%

    Description: Sertraline HCl (formerly CP 51,974-1; CP 51974-1; CP-51,974; trade names: Sealdin; Adjuvin; Atruline; Gladem; Tatig; Tresleen; Zoloft), the hydrochloride salt of Sertraline, is a potent and marketed antidepressant drug acting as a 5-HT serotonin receptor antagonist with Ki of 13 nM. Sertraline is primarily a serotonin reuptake inhibitor (SRI) with a binding affinity towards the serotonin transporter of Ki=2.8 nM. Sertraline exhibits better selectivity for inhibiting 5-HT uptake relative to NE uptake than fluvoxamine, zimelidine, norzimelidine, fluoxetine or chlorimipramine. However, Sertraline is less selective for blocking 5-HT uptake, relative to DA uptake than these agents. Sertraline is also a dopamine reuptake inhibitor, (<50 nmol/L). However, this is not considered a tight binding, and this action is only 10% of its potency as a monoamine reuptake inhibitor. It is a σ1 receptor agonist with 5% of its SRI potency, and an α1-adrenoreceptor antagonist with 1–10% of its SRI potency.

    References: J Pharmacol Exp Ther. 1983 Sep;226(3):686-700.

    Related CAS: 79617-96-2 (free base) 79559-97-0 (HCl)

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    Molecular Weight (MW)342.69 
    FormulaC17H17Cl2N.HCl 
    CAS No.79559-97-0  (HCl); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 69 mg/mL (201.3 mM) 
    Water: <1 mg/mL
    Ethanol: 15 mg/mL (43.8 mM)
    Solubility (In vivo)30% PEG400+0.5% Tween80+5% Propylene glycol: 5 mg/mL 
    SynonymsCP-51974-1 HCl; CP51974-1 HCl; Sertraline Hydrochloride; Sertraline HCl; Sealdin; Adjuvin; Atruline; CP 51,974-1; Cp-51,974-1; CP 51974-1 HCl;  CP 51,974; CP51,974; CP-51,974; Gladem; Tatig; Tresleen; Zoloft.


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    In Vitro

    In vitro activity: Sertraline exhibits better selectivity for inhibiting 5-HT uptake relative to NE uptake than fluvoxamine, zimelidine, norzimelidine, fluoxetine or chlorimipramine. However, Sertraline is less selective for blocking 5-HT uptake, relative to DA uptake than these agents.

    In VivoSertraline HCl (32μmol/kg i.p.) inhibits serotonin uptake into striatal synaptosomes from rats by more than 50%. Sertraline HCl is 6 times more potent than chlorimipramine and 60 times more potent than amitriptyline in reversing the 5-HT depletion elicited by PCA. Acute and repeated dosing of sertraline decreased serotonin content of whole blood. Sertraline HCl strongly reduces immobility of mice in the Porsolt swim test for antidepressants. After repeated dosing in rats, sertraline HCl diminishes the cyclic AMP response of limbic forebrain adenylate cyclase to norepinephnne, as well as the binding of [3H]dihydroalprenolol to cortical membranes. 
    Animal modelRats
    Formulation & Dosage32μmol/kg i.p.
    References J Pharmacol Exp Ther. 1983 Sep;226(3):686-700.


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

     
    Sertraline HCl
    Sertraline increases survival and improves motor behavioral performance, but does not affect body weight loss in HD mice. Neurobiol Dis. 2008 Jun; 30(3): 312–322.


    Sertraline HCl
    Sertraline normalizes BDNF protein levels and serotonin (5-HT) levels, and upregulates HSP70 and Bcl-2 levels. Neurobiol Dis. 2008 Jun; 30(3): 312–322.


     

     
    Sertraline HCl
    Sertraline reduces brain atrophy but not huntingtin inclusions in N171-82Q HD mice. Neurobiol Dis. 2008 Jun; 30(3): 312–322.
     
    Sertraline HCl
    Sertraline increases neurogenesis in subgranular zone (SGZ) of dentate gyrus in HD mice and control mice.


    Sertraline HCl
    Sertraline increases neurogenesis in subventricular zone (SVZ) of mice. Neurobiol Dis. 2008 Jun; 30(3): 312–322.


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