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MedChemExpress - Model Eletriptan hydrobromide -177834-92-3
MCE products for research use only. We do not sell to patients.
Eletriptan hydrobromide
MCE China：Eletriptan hydrobromide
Brand：MedChemExpress (MCE)
Cat. No.HY-A0010
CAS：177834-92-3
Synonyms：Eletriptan HBr; UK-116044 hydrobromide
Purity：99.81%
Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Shipping：Room temperature in continental US; may vary elsewhere.
Description：Eletriptan hydrobromide (Eletriptan HBr) is a 5-HT1B and 5-HT1D receptor agonist with antimigraine activity, with Ki of 0.92 nM and 3.14 nM, respectively.
In Vivo：Eletriptan (1-1000 μg/kg; i.v.; after a 60-minute stabilization period, dosed at 5-minute intervals with readings taken every 30 seconds) hydrobromide dose-dependently reduces carotid blood flow in anesthetized dogs[1]. Eletriptan (30-300 μg/kg; i.v.) hydrobromide dose-dependently inhibits dural plasma protein extravasation in anesthetized rats and rapidly and completely inhibits plasma protein extravasation from the dura mater at a dose of 100 μg/kg[1].
IC50 & Target：5-HT1B Receptor 0.92 nM (Ki) 5-HT1D Receptor 3.14 nM (Ki)
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References：
[1]. Napier C, et al. Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. Eur J Pharmacol, 1999, 368(2-3), 259-268. [Content Brief]
[2]. MaassenVanDenBrink A, et al. Craniovascular selectivity of eletriptan and sumatriptan in human isolated blood vessels. Neurology, 2000, 55(10), 1524-1530. [Content Brief]
[3]. Gupta P, et al. The in vivo pharmacological profile of eletriptan (UK-116,044): a potent and novel 5-HT(1B/1D) receptor agonist. Eur J Pharmacol, 2000, 398(1), 73-81. [Content Brief]
[4]. Hoskin KL, et al. The 5-hydroxytryptamine1B/1D/1F receptor agonists eletriptan and naratriptan inhibit trigeminovascular input to the nucleus tractus solitarius in the cat. Brain Res, 2004, 998(1), 91-99. [Content Brief]
[5]. Willems E, et al. Porcine carotid vascular effects of eletriptan (UK-116,044): a new 5-HT1B/1D receptor agonist with anti-migraine activity[J]. Naunyn-Schmiedeberg's archives of pharmacology, 1998, 358: 212-219. [Content Brief]
[6]. Johnson D E, et al. Serotonergic effects and extracellular brain levels of eletriptan, zolmitriptan and sumatriptan in rat brain[J]. European journal of pharmacology, 2001, 425(3): 203-210. [Content Brief]
Brand introduction:
• MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
• More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
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• It has a professional experimental center and strict quality control and verification system；
• Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
• The biological activity of the products has been verified by the experiments of customers in various countries；
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