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Eletriptan HBr
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Eletriptan HBr图片
CAS NO:177834-92-3
规格:≥98%
包装与价格:
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
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[C@@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.
实验参考方法
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.