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    Lorcaserin HCl
    Lorcaserin 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 #: V1032
    CAS #: 846589-98-8 Purity ≥98%

    Description: Lorcaserin HCl (Belviq Xr; APD-356; APD356; Lorqess), the hydrochloride salt of Lorcaserin which is a marketed weight-loss drug, is a potent and selective full agonist of human 5-HT2C (serotonin) receptor with Ki of 15 nM. It reduces appetite by activating 5-HT2C receptor the hypothalamus, which is known to control appetite.

    References: J Pharmacol Exp Ther. 2008 May;325(2):577-87; J Pharmacol Exp Ther. 2011 Sep;338(3):890-6. 

    Related CAS#: 616202-92-7 (free base); 856681-05-5 (HCl hydrate); 1361572-46-4 (Lorcaserin sulfamate)

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    Molecular Weight (MW)232.15
    FormulaC11H14ClN.HCl 
    CAS No.846589-98-8 (HCl);
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 46 mg/mL (198.1 mM) 
    Water: 46 mg/mL (198.1 mM) 
    Ethanol: 46 mg/mL (198.1 mM) 
    SMILESC[[email protected]]1CNCCC2=CC=C(Cl)C=C12.[H]Cl
    SynonymsAPD 356; Lorcaserin hydrochloride; Belviq Xr; Lorcaserin HCl; APD-356; APD356; Lorqess. 


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    In Vitro

    In vitro activity: Lorcaserin exhibits higher affinity for human 5-HT2C than to 5-HT 5-HT2A (7.5-fold selective, Ki=112 nM) and 5-HT2B (11.6-fold selective, Ki=174 nM). Lorcaserin possesses agonist activity at all three human 5-HT2 receptors. Lorcaserin is 18-fold more potent at human 5-HT2C (EC50= 9 nM) than at human 5-HT2A (EC50= 168 nM), and it is 104-fold more potent at human 5-HT2C than human 5-HT2B (EC50= 943 nM). Lorcaserin shows full agonist activity at the human 5-HT2C and 5-HT2B receptors and partial agonist activity at the human 5-HT2A receptor (100%, 100% and 75% of the maximal response elicited by serotonin, respectively). Lorcaserin does not compete for binding of ligands to serotonin, dopamine, and norepinephrine transporters. Lorcaserin does not stimulate norepinephrine, dopamine, or serotonin release from rat synaptosomes at submicromolar concentrations. Lorcaserin weakly inhibits norepinephrine (EC50= 2500 nM), serotonin (EC50= 1400 nM), and dopamine (EC50= 12,000 nM) uptake.


    In VivoLorcaserin produces dose-dependent reductions in food intake and body weight gain during the 4-week study. Lorcaserin (18 mg/kg) significantly increases resting and penile grooming, and has no effects on wet dog shakes, and back muscle contractions of rats. Lorcaserin short-term administration (0.3125-20 mg/kg) significantly reduces nicotine self-administration in female rats. Long-term Lorcaserin (0.625 mg/kg) also significantly reduces nicotine self-administration over a 2-week period of repeated injections. 
    Animal modelRats
    Formulation & Dosage0.3125-20 mg/kg; injections
    ReferencesJ Pharmacol Exp Ther. 2008 May;325(2):577-87; J Pharmacol Exp Ther. 2011 Sep;338(3):890-6.  


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

     
    Lorcaserin HCl
    A, short-term dose-effect function of the higher dose range of lorcaserin on nicotine-self-administration (mean ± S.E.M.). J Pharmacol Exp Ther. 2011 Sep;338(3):890-6. 
     
    Lorcaserin HCl
    A, short-term dose-effect function of the lower dose range of lorcaserin on nicotine-self-administration (mean ± S.E.M.). J Pharmacol Exp Ther. 2011 Sep;338(3):890-6. 
     

    Lorcaserin HCl

    A, chronic lorcaserin administration effect on locomotor activity over 2 weeks of treatment averaged over 12 5-min blocks. J Pharmacol Exp Ther. 2011 Sep;338(3):890-6. 


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