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Eletriptan HBr

氢溴酸依来曲普坦,UK-116044,UK116044,UK 116044

Eletriptan HBr 是一种选择性的5-羟色胺1B和1D受体激动剂，Ki值分别为0.92 nM和3.14 nM。

目录号
EY0304
EY0304
EY0304
EY0304
纯度
99.69%
99.69%
99.69%
99.69%
规格
1 mg
5 mg
10 mg
50 mg
原价
220
570
725
2760
售价
220
570
725
2760
库存
现货
现货
现货
现货
订购
订购
订购
订购
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  • 生物活性

    Eletriptan is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Gupta 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 73.
    [2] Napier et al (1999) 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. 368 259.
    [3] Ponnuru VS, Challa BR, Nadendla R.Quantitative analysis of eletriptan in human plasma by HPLC-MS/MS and its application to pharmacokinetic study.Anal Bioanal Chem. 2011 Nov;401(8):2539-48. Epub 2011 Sep 3.

    分子式
    C22H26N2O2S.HBr    		 分子量
    463.43    		 CAS号
    177834-92-3    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    100 mM    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT00259649 Migraine Drug: eletriptan University of Pittsburgh|Pfizer Phase 4 2004-08-01 2011-07-01
    NCT00174395 Migraine Drug: eletriptan Pfizer Phase 4 2005-03-01 2007-10-31
    NCT01859481 Migraine Without Aura|Migraine With Aura Drug: Placebo|Drug: Eletriptan HBr 40 mg|Drug: Eletriptan HBr 80 mg Pfizer Phase 3 2000-03-01 2013-05-17
    NCT01276977 Acute Migraine|Migraine Headache|Headache Disorders Drug: Zolmitriptan 5 mg Nasal Spray|Drug: Eletriptan 40 mg tablet California Medical Clinic for Headache 2008-04-01 2011-01-13
    NCT00871806 Healthy Volunteers Drug: Commercial tablet with water|Drug: ODT #1 without water|Drug: ODT #2 without water|Drug: ODT #1 with water|Drug: ODT #2 with water Pfizer Phase 1 2009-04-01 2010-04-22
    NCT01989936 Migraine With or Without Aura Drug: Placebo|Drug: Eletriptan 40 mg|Drug: Eletriptan 80 mg Pfizer Phase 3 1999-01-01 2013-11-20
    NCT00632385 Migraine Drug: Eletriptan Pfizer Phase 4 2003-01-01 2011-04-22
    NCT00385008 Migraine Disorders Drug: Combination Product (sumatriptan succinate / naproxen sodium)|Drug: RELPAX(eletriptan) 40mg Tablet GlaxoSmithKline Phase 3 2006-09-01 2016-10-24
    NCT00634985 Migraine Drug: eletriptan Pfizer Phase 4 2002-11-01 2011-04-22
    NCT01978496 Migraine With or Without Aura Drug: Placebo|Drug: Eletriptan 20 mg|Drug: Eletriptan 40 mg|Drug: Eletriptan 80 mg Pfizer Phase 3 1996-07-01 2013-11-11
    NCT01139515 Healthy Drug: Eletriptan commercial tablet|Drug: Eletriptan commercial tablet|Drug: Eletriptan commercial tablet|Drug: Eletriptan commercial tablet Pfizer Phase 1 2010-07-01 2011-06-13
    NCT01986088 Migraine With or Without Aura Drug: Placebo|Drug: Eletriptan 40 mg|Drug: Eletriptan 80 mg|Drug: Sumatriptan 50 mg|Drug: Sumatriptan 100 mg Pfizer Phase 3 1996-11-01 2013-11-11
    NCT01986270 Migraine With or Without Aura Drug: Placebo|Drug: Eletriptan 40 mg|Drug: Eletriptan 80 mg|Drug: Sumatriptan 25 mg|Drug: Sumatriptan 50 mg Pfizer Phase 3 1996-12-01 2013-11-11
    NCT00751803 Migraine Disorders Drug: BI 44370 TA Low Dose|Drug: Eletriptan|Drug: Placebo|Drug: BI 44370 TA Medium Dose Boehringer Ingelheim Phase 2 2008-08-01 2014-11-12
    NCT01435941 Migraine Disorders Drug: Non-steroidal anti-inflammatory drug (NSAID)|Drug: Triptan GlaxoSmithKline 2009-09-01 2011-09-21
    NCT01381497 Migraine Disorders Drug: Combination therapy of sumatriptan and naproxen sodium (SumaRT/Nap)|Drug: Triptan monotherapy GlaxoSmithKline 2010-03-01 2012-08-23
    NCT01381523 Migraine Disorders Drug: Combination therapy with sumatriptan and naproxen sodium (SumaRT/Nap)|Drug: Single-entity oral triptans GlaxoSmithKline 2010-11-01 2013-02-21
    NCT01332500 Migraine Disorders Drug: Sumatriptan/Naproxen combination|Drug: other oral triptans GlaxoSmithKline 2009-07-01 2011-04-19
    NCT01086358 Workplace Migraine Treatment Drug: Usual prescribed triptan|Drug: Treximet for migraine treatment The Cleveland Clinic|Pernix Theraputics LLC Phase 4 2009-09-01 2016-08-10

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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