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    Rizatriptan Benzoate (MK-462 Benzoate)
    Rizatriptan Benzoate (MK-462 Benzoate)

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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 #: V0979
    CAS #: 145202-66-0Purity ≥98%

    Description: Rizatriptan Benzoate (Maxalt; formerly MK 0462; MK 462) is a potent and selective agonist at serotonin 5-HT1B and 5-HT1D receptors with anti-migraine activity. It can be potentially used for the treatment of acute migraines.

    References: Br J Pharmacol. 2001 Aug;133(7):1029-34; Eur J Pharmacol. 1997 Jun 5;328(1):61-4.

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    Molecular Weight (MW)391.47 
    FormulaC22H25N5O2 
    CAS No.145202-66-0 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 20 mg/mL (51.08 mM) 
    Water: 46 mg/mL (117.5 mM)   
    Ethanol: <1 mg/mL
    SMILES CodeCN(C)CCC1=CNC2=C1C=C(C=C2)CN3C=NC=N3.C1=CC=C(C=C1)C(=O)O
    SynonymsMK-462 Benzoate;izatriptan Benzoate; MK-0462; 2-(5-((1H-1,2,4-TRIAZOL-1-YL)METHYL)-1H-INDOL-3-YL)-N,N-DIMETHYLETHANAMINE BENZOATE; MK 462; rizatriptan benzoate; Maxalt; MK 0462; MK 462;


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    In Vitro

    In vitro activity: Rizatriptan Benzoate (also known as MK-462 Benzoate) is a novel, potent and selective agonist at serotonin 5-HT1B and 5-HT1D receptors, it can be potentially used to treat acute migraine attacks. 

    In VivoRizatriptan blocks neurogenic vasodilation via an action on 5-HT(1D) receptors located on perivascular trigeminal nerves to inhibit CGRP release in anaesthetized guinea-pigs. Rizatriptan evokes a transient reduction in dural blood vessel diameter which recovered to baseline values within 10 min in anaesthetized guinea-pigs. Rizatriptan significantly inhibits dural plasma protein extravasation produced by high intensity electrical stimulation of the trigeminal ganglion. Rizatriptan significantly reduces electrically stimulated dural vasodilation in anaesthetised rats. Rizatriptan Benzoate significantly reduced SP mRNA levels in the midbrains of normal and model group rats, indicating that Rizatriptan Benzoate can downregulate SP gene expression in the rat midbrain. Rizatriptan Benzoate significantly reduces midbrain PENK mRNA expression, decreasing the levels of midbrain met-enkephalin and leu-enkephalin, and thereby weakening the analgesic effects of the endogenous pain modulatory system in rat model of migraine.
    Animal model Rats
    Formulation & Dosage N/A
    ReferencesEur J Pharmacol. 1997 Jun 5;328(1):61-4. 


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

     
    Rizatriptan Benzoate
    Effects of (a) 0.3 mg kg−1 i.v. human-αCGRP(8-37) on neurogenic dural vasodilation and (b) rizatriptan on neurogenic or rat-αCGRP-evoked dural vasodilation in anaesthetized guinea-pigs. Br J Pharmacol. 2001 Aug;133(7):1029-34.
     
    Rizatriptan Benzoate
    Effects of (a) PNU-142633 and (b) LY334370 on neurogenic dural vasodilation in anaesthetized guinea-pigs. Br J Pharmacol. 2001 Aug;133(7):1029-34.


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