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    Eletriptan HBr
    Eletriptan HBr

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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 #: V0995
    CAS #: 177834-92-3Purity ≥98%

    Description: Eletriptan (formerly UK 116044; UK-116,044; UK-116,044-04; trade name Relpax), a triptan class of medication used for treatment of migraine headaches, is a potent and selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively. Eletriptan is used as an abortive medication.

    References: Eur J Pharmacol. 1999 Mar 5;368(2-3):259-68; Eur J Pharmacol. 2000 Jun 9;398(1):73-81.

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    Molecular Weight (MW)463.43 
    FormulaC22H26N2O2S.HBr 
    CAS No.177834-92-3 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 93 mg/mL (200.7 mM) 
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: 5-[2-(benzenesulfonyl)ethyl]-3-[[(2R)-1-methylpyrrolidin-2-yl]methyl]-1H-indole;hydrobromide

    InChi Key: UTINOWOSWSPFLJ-FSRHSHDFSA-N

    InChi Code: InChI=1S/C22H26N2O2S.BrH/c1-24-12-5-6-19(24)15-18-16-23-22-10-9-17(14-21(18)22)11-13-27(25,26)20-7-3-2-4-8-20;/h2-4,7-10,14,16,19,23H,5-6,11-13,15H2,1H3;1H/t19-;/m1./s1

    SMILES Code: CN1CCC[[email protected]@H]1CC2=CNC3=C2C=C(C=C3)CCS(=O)(=O)C4=CC=CC=C4.Br

    SynonymsUK-116044 HBr; Eletriptan; UK 116044; UK-116,044; UK-116,044-04; UNII-22QOO9B8KI.


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    In Vitro

    In vitro activity: [3H]Eletriptan has a total number of binding sites (Bmax) of 2478 fmol/mg and 1576 fmol/mg for 5-HT1B and 5-HT1D, respectively. [3H]Eletriptan has a significantly faster association rate (K(on) 0.249/min/nM) than [3H]sumatriptan (K(on) 0.024/min/nM) and a significantly slower off-rate (K(off) 0.027/min compared to 0.037/min for [3H]sumatriptan). Eletriptan induces concentration-dependent contractions of meningeal artery, coronary artery, and saphenous vein. The potency of Eletriptan is higher in meningeal artery than in coronary artery (86-fold) or saphenous vein (66-fold). The predicted contraction by Eletriptan (40 mg and 80 mg) and sumatriptan (100 mg) at free C(max) observed in clinical trials is similar in meningeal artery.

    In VivoEletriptan (<1000 mg/kg, i.v.) produces a dose-dependent reduction of carotid arterial blood flow in the anaesthetised dog. Eletriptan reduces coronary artery diameter with ED50 value of 63 mg/kg in the anaesthetised dog. Eletriptan (<300 mg/kg, i.v.) administered prior to electrical stimulation of the trigeminal ganglion produces a dose-related and complete inhibition of plasma protein extravasation in the dura mater rats. Eletriptan (100 mg/kg, i.v.) produces a complete inhibition of plasma protein extravasation in rat dura mater. Headache response rates are 24% for placebo; 54% for Eletriptan (20 mg);65% for Eletriptan (40 mg);and 77% for Eletriptan (80 mg) at the primary endpoint (2 hours after dosing) in patients with migraine. Headache-free rates at 2 hours are 6% for placebo, 29% for Eletriptan (40 mg) and 37% for Eletriptan (80 mg) at the primary endpoint (2 hours after dosing) in patients with migraine. Eletriptan is well tolerated, and the majority of adverse events are mild or moderate in intensity and transient in patients with migraine. Iontophoretic ejection (50 nA) of Eletriptan suppresses the response in 75% of cells and causes an average suppression of cell firing of 42% in cats. 
    Animal modelRats
    Formulation & Dosage<1000 mg/kg, i.v.
    References

    Eur J Pharmacol. 1999 Mar 5;368(2-3):259-68; Eur J Pharmacol. 2000 Jun 9;398(1):73-81. 


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

     
    Eletriptan HBr
    Proportion of patients reporting satisfaction as ‘good-to-excellent’: comparison of eletriptan 40 mg with previous migraine treatment (total sample, n = 437). Int J Clin Pract. 2007 Oct; 61(10): 1677–1685.
     
    Eletriptan HBr
    Subgroup analysis: proportion of patients reporting ‘fair-to-very poor’ response to previous migraine treatment who reported satisfaction as ‘good-to-excellent’ when switched to eletriptan 40 mg. Int J Clin Pract. 2007 Oct; 61(10): 1677–1685.
     Eletriptan HBr


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