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    Ketanserin (R41468)
    Ketanserin (R41468)

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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 #: V0964
    CAS #: 74050-98-9Purity ≥98%

    Description: Ketanserin (R41468; Vulketan; R-41468), an aprroved antihypertensive drug, is a potent and specific 5-HT2A serotonin receptor antagonist with a Ki of 2.5 nM for rat and human 5-HT2A. It can also be used to discriminate between 5-HT1D and 5-HT1B receptor subtypes. Ketanserin inhibits the contractions of rat caudal arteries and canine saphenous veins caused by postjunctional alpha adrenergic activation.

    References: J Pharmacol Exp Ther. 1981 Jul;218(1):217-30; Neuropharmacology. 1985 Apr;24(4):265-73.

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    Molecular Weight (MW)395.43
    FormulaC22H22FN3O3
    CAS No.74050-98-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 2 mg/mL (5.1 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    SMILES CodeO=C(N1CCN2CCC(C(C3=CC=C(F)C=C3)=O)CC2)NC4=C(C=CC=C4)C1=O
    SynonymsR41468;  R 41468; Vulketan; R-41468 


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    In Vitro

    In vitro activity: Ketanserin causes a dose-dependent inhibition on the contractile responses to 5-hydroxytryptamine of isolated rat caudal artery, canine basilar, carotid, coronary and gastrosplenic arteries, canine gastrosplenic veins and canine saphenous veins. Ketanserin inhibits the contractions of rat caudal arteries and canine saphenous veins caused by postjunctional alpha adrenergic activation. Ketanserin depresses and in certain experiments reverses the vasoconstrictor response to 5-hydroxytryptamine in the perfused guinea-pig stomach. Ketanserin is found to attenuate the excitatory responses produced by norepinephrine, an alpha 1-adrenoceptor-mediated response, in the lateral geniculate nucleus. Ketanserin potentiates rather than attenuates, the inhibitory effect of 5-HT in the lateral geniculate nucleus. Ketanserin significantly prolongs action potential duration (APD) at 50% repolarization by 218% and APD at 90% repolarization by 256% with no significant effect on other action potential parameters in rat ventricular myocytes. Ketanserin results in a concentration- and time-dependent inhibition of charge area of Ito evaluated by integration with an EC50 of 8.3 μM. Ketanserin also blocks Ito and sustained current (ISus) in a dose-dependent manner with an EC50 of 11.2 μM and has no significant effect on both the inward rectifier potassium current and the L-type calcium current.


    Cell Assay: The established HEK 293 cell line stably expressing hERG channels is cultured in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% foetal bovine serum, 400 μg/mL G418. The HEK 293 cell line stably expressing recombinant human cardiac KCNQ1/KCNE1 channel current (IKs) is maintained in DMEM containing 10% foetal bovine serum and 100 μg/mL hygromycin. Cells used for electrophysiology are seeded on a glass coverslip. The mutant hERG channels are constructed, and are transiently expressed in HEK 293 cells using 10 μL of Lipofectamine 2000 with 4 μg of hERG mutant cDNA in pCDNA3 vector.

    In VivoKetanserin produces dose-dependent antinociception in the hot-plate and acetic acid-induced writhing tests with ED50 values (95% confidence limit) of 1.51 and 0.62 mg/kg, respectively, but is without any significant effect on the tail-flick test.
    Animal modelRats: A total of 155 specific-pathogen-free 2-month-old male Sprague-Dawley rats, weighing 180-220 g, are used. The rats are randomly divided into the following six groups: 5-HT1A receptor agonist (8-OH-DPAT) PS group (DPAT-PS group, n=30); 5-HT1A receptor antagonist (MDL73005) PS group (MDL-PS group, n=30); 5-HT2A receptor agonist (DOI) PS group (DOI-PS group, n=30); 5-HT2A receptor antagonist (Ketanserin) PS group (Ketan-PS group, n=30); the solvent control no-stress group (0.9% physiological saline group, CON group); and the PS only group (PS group, n=30). The DPAT-PS, MDL-PS, DOI-PS, Ketan-PS and PS groups are further divided into six subgroups (n=5 each) according to the time between the stress and analysis; immediately after stress, and 0.5, 1, 2, 6 and 24 hours after stress. The CON group (n=5) receive normal feed. For the Ketan-PS group, Ketanserin, dissolved in 0.9% physiological saline, is injected intraperitoneally at 5 mg/kg at 1 hour before each stress exposure.
    Formulation & Dosage5 mg/kg
    References

    J Pharmacol Exp Ther. 1981 Jul;218(1):217-30; Neuropharmacology. 1985 Apr;24(4):265-73.


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

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