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    LY310762
    LY310762

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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 #: V0981
    CAS #: 192927-92-7Purity ≥98%

    Description: LY310762 (LY-310762; LY 310762) is a potent 5-HT1D serotonin receptor antagonist with important biological activity. It inhibits 5-HT1D with a Ki of 249 nM and shows good selectivity over the closely related 5-HT isoforms.

    References: Eur J Pharmacol. 2004 Jun 16;493(1-3):85-93; Br J Pharmacol. 2012 Sep;167(2):356-67.

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    Molecular Weight (MW)430.94 
    FormulaC24H27FN2O2.HCl 
    CAS No.192927-92-7 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: <1 mg/mL
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    SMILES Code O=C1N(CCN2CCC(C(C3=CC=C(F)C=C3)=O)CC2)C4=C(C=CC=C4)C1(C)C.[H]Cl
    Synonyms LY310762; LY 310762; LY-310762; LY310762 HCl.


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    In Vitro

    In vitro activity: LY310762 has a higher affinity for the guinea pig 5-HT1D receptor than for the 5-HT1B receptor. LY310762 potentiates the potassium-induced [3H]5-HT outflow from guinea pig cortical slices with an EC50 of 30 nM. The maximum potentiation of the potassium-induced outflow which is obtained with LY310762 is about 40%. LY310762 blocks the decreased EPSC amplitude induced by Sumatriptan.


    Kinase Assay: LY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, having a weaker affinity for 5-HT1B receptor.  


    Cell Assay: LY310762 has a higher affinity for the guinea pig 5-HT1D receptor than for the 5-HT1B receptor. LY310762 potentiates the potassium-induced [3H]5-HT outflow from guinea pig cortical slices with an EC50 of 30 nM. The maximum potentiation of the potassium-induced outflow which is obtained with LY310762 is about 40%. LY310762 blocks the decreased EPSC amplitude induced by Sumatriptan.

    In VivoSystemic administration of LY310762 (10 mg/kg i.p.) produces a further significant enhancement in the 5-HT response to fluoxetine (20 mg/kg i.p.) when compared to animals receiving a control vehicle injection. In fluoxetine treated animals, levels of 5-HT increases from 312±43% to a maximum of 683% after LY310762. In control animals, levels of 5-HT remains unchanged (250%). LY310762 administered alone also significantly increases basal levels of 5-HT above vehicle controls, reaching a maximum of 258% compared to the pre-injection control. 
    Animal modelAnimals
    Formulation & Dosage10, 20 mg/kg i.p.
    ReferencesEur J Pharmacol. 2004 Jun 16;493(1-3):85-93; Br J Pharmacol. 2012 Sep;167(2):356-67. 


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

    LY310762
    Effects of 5-HT1B and 5-HT1D receptor antagonists on the CP93129-induced decrease in EPSCs. Br J Pharmacol. 2012 Sep;167(2):356-67.
     
    LY310762
    Effects of sumatriptan on glutamatergic EPSCs. Br J Pharmacol. 2012 Sep;167(2):356-67.


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