Eletriptan
(Synonyms: 依来曲普坦,UK-116044) 目录号 : GC43594
An agonist of 5-HT1B and 5-HT1D receptors
Cas No.:143322-58-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Eletriptan is an agonist of the serotonin (5-HT) receptor types 5-HT1B and 5-HT1D. It inhibits forskolin-induced cAMP accumulation in and induces vasoconstriction of isolated rabbit common carotid artery rings (pD2s = 7.6 and 4.9, respectively), an effect that can be blocked by the 5-HT1B antagonist SB216641 but not the 5-HT1D antagonist BRL15572. Eletriptan preferentially induces constriction of isolated human cerebral over coronary arteries (EC50s = 15.8 and 1,995 nM, respectively). Formulations containing eletriptan have been used in the treatment of migraine headache.
| Cas No. | 143322-58-1 | SDF | |
| 别名 | 依来曲普坦,UK-116044 | ||
| Canonical SMILES | CN(CCC1)[C@H]1CC2=CNC3=CC=C(CCS(C4=CC=CC=C4)(=O)=O)C=C32 | ||
| 分子式 | C22H26N2O2S | 分子量 | 382.5 |
| 溶解度 | DMF: 10 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 10 mg/ml,Ethanol: 0.1 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6144 mL | 13.0719 mL | 26.1438 mL |
| 5 mM | 0.5229 mL | 2.6144 mL | 5.2288 mL |
| 10 mM | 0.2614 mL | 1.3072 mL | 2.6144 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Eletriptan
Expert Opin Investig Drugs 2001 Oct;10(10):1869-74.PMID:11772292DOI:10.1517/13543784.10.10.1869.
Eletriptan (Relpax, Pfizer) is one of a group of anti-migraine medications commonly referred to as 'triptans'. It is a potent serotonin agonist at the 5-HT(1B/1D) receptor and is indicated for the acute treatment of migraine headaches. Eletriptan is administered orally. It is rapidly absorbed and has a bioavailability of 50% compared to 14% for sumatriptan. The relatively high lipophilicity of Eletriptan compared to sumatriptan may explain its faster oral absorption and shorter time to onset of action. Results from comparative studies between oral Eletriptan and sumatriptan indicate that Eletriptan 80 mg was superior to sumatriptan 100 mg in onset of action, headache response rate, pain free response rate and relief of associated migraine symptoms at the 1 or 2 h time intervals. Although there was a modest increase in adverse events with Eletriptan 80 mg than with sumatriptan 100 mg, Eletriptan received a high patient acceptability rating (84%).
Eletriptan
Expert Opin Drug Metab Toxicol 2009 Dec;5(12):1587-98.PMID:19929447DOI:10.1517/17425250903410226.
Migraine is a multifactorial chronic central nervous system disorder, characterized by recurrent disabling attacks of moderate-to-severe headache. Symptomatic acute treatment of migraine should provide rapid and effective relief of the headache pain. The introduction of the 5-HT(1B/1D) receptor agonists (triptans) expanded the armamentarium for acute migraine pain treatment. Eletriptan is a second-generation triptan with favorable bioavailability and half-life, a high affinity for 5-HT(1B/1D) receptors and selectivity for cranial arteries. Eletriptan (40 and 80 mg) has been shown to be effective as early as 30 min after administration and well tolerated when compared to placebo. In comparative clinical trials, Eletriptan 40 and 80 mg were superior or equivalent to other triptans and have shown a very high safety and tolerability profile across the studies performed. Eletriptan showed the most favorable cost-effectiveness profile when compared with other agents in its class.
Eletriptan review
Expert Opin Pharmacother 2005 Apr;6(4):625-30.PMID:15934888DOI:10.1517/14656566.6.4.625.
Eletriptan is a selective, high affinity serotonin 5-HT(1B/1D)-receptor agonist which is rapidly absorbed and has a long half-life in plasma. Eletriptan has been shown to be effective and well tolerated in randomised, double-blind, placebo-controlled acute migraine trials and long-term open-label trials. Eletriptan maintains a consistency of response across three attacks and patients continue to respond to Eletriptan for at least up to 1 year. Eletriptan has been compared with sumatriptan, zolmitriptan, naratriptan and ergotamine/caffeine in placebo-controlled, randomised, head-to-head trials, and has shown better efficacy with similar adverse events. In a large triptan meta-analysis, including 53 trials and > 24,000 patients, Eletriptan 80 mg showed better efficacy, similar consistency but lower tolerability compared with sumatriptan 100 mg. Eletriptan has also shown efficacy in difficult-to-treat patients who were dissatisfied with their previous treatment with sumatriptan, rizatriptan, nonsteroidal anti-inflammatory drugs or Excedrin.
Eletriptan: a review of its use in the acute treatment of migraine
Drugs 2006;66(8):1129-49.PMID:16789799DOI:10.2165/00003495-200666080-00010.
Eletriptan (Relpax) is an orally administered, lipophilic, highly selective serotonin 5-HT(1B/1D) receptor agonist ('triptan') that is effective in the acute treatment of moderate to severe migraine attacks in adults. It has a rapid onset of action and demonstrates superiority over placebo as early as 30 minutes after the administration of a single 40 or 80 mg oral dose. The efficacy of Eletriptan 20 mg was similar to that of sumatriptan 100 mg, while Eletriptan 40 and 80 mg displayed greater efficacy than sumatriptan 50 or 100 mg for most endpoints. Eletriptan 40 mg was generally superior to naratriptan 2.5 mg and equivalent to almotriptan 12.5 mg, rizatriptan 10 mg and zolmitriptan 2.5 mg, while Eletriptan 80 mg was superior to zolmitriptan 2.5 mg for most efficacy parameters. Eletriptan 40 and 80 mg were consistently superior to ergotamine/caffeine. Eletriptan is generally well tolerated, reduces time lost from normal activities, improves patients' health-related quality of life and appears to be at least as, if not more, cost effective than sumatriptan. Eletriptan is therefore a useful addition to the triptan family and a first-line treatment option in the acute management of migraine attacks.
Eletriptan for acute migraine
Cochrane Database Syst Rev 2001;(3):CD003224.PMID:11687056DOI:10.1002/14651858.CD003224.
Background: Eletriptan (Relpax) is a new triptan soon to be made available by prescription for the treatment of acute migraine. Currently five triptans are available by prescription and more are under development. In light of the many drugs for treating acute migraine, there is a need for evidence-based assessments to help determine the relative efficacy and harm of these treatments. Objectives: To determine the efficacy of Eletriptan for treating a single migraine attack using the outcomes of headache response and pain-free response at 0.5, 1, 2 and 4 hours, and sustained relief over 24 hours. To express efficacy in terms of number-needed-to-treat (NNT). To determine the adverse effects of a single dose of Eletriptan and express this in terms of number-needed-to-harm (NNH). To allow for the comparison of the efficacy of Eletriptan with other migraine treatments evaluated systematically in the same way. Search strategy: Data from all Phase III randomised placebo-controlled trials were made available by the manufacturer, Pfizer Inc. To date, these trials comprise the only data on Eletriptan relevant to this review in a published or unpublished form; thus, searches of electronic databases for further trials of Eletriptan were not conducted. Selection criteria: Trials of Eletriptan for acute migraine; randomised allocation to treatment groups, including a placebo group; double-blind design; International Headache Society diagnostic criteria for migraine with or without aura; single migraine attack; single-dose treatment at standard doses; adult population; baseline pain of moderate or severe intensity using a 4-point standardised rating scale (0 = no pain, 1 = mild pain, 2 = moderate pain and 3 = severe pain); and dichotomous or percentage data for at least one of the main efficacy outcomes. Data collection and analysis: Trials were scored for quality and data extracted by two independent reviewers. Dichotomous or percentage data were extracted and pooled to calculate the relative benefit (RB) or relative risk (RR) and NNTs or NNHs for a number of outcomes for Eletriptan 20 mg, 40 mg and 80 mg. The main outcomes considered were headache response at 1 and 2 hours, pain-free response at 2 hours, sustained relief over 24 hours and adverse effects. Minor outcomes considered were headache response at 0.5 and 4 hours, and pain-free response at 0.5, 1 and 4 hours. Main results: Six trials met the inclusion criteria. Significant benefit of Eletriptan over placebo was shown for Eletriptan 20 mg, 40 mg and 80 mg for the primary efficacy outcomes of headache response and pain-free response at 2 hours. For headache response at 2 hours, the NNTs (with 95% confidence intervals) were 4.4 (3.4 to 6.2), 2.9 (2.6 to 3.3) and 2.6 (2.4 to 3.0) for Eletriptan 20 mg, 40 mg and 80 mg, respectively. For pain-free response at 2 hours, the NNTs were 9.9 (6.9 to 18), 4.5 (4.0 to 5.1) and 3.7 (3.4 to 4.2), for Eletriptan 20 mg, 40 and 80 mg, respectively. There was no significant difference in the incidence of major adverse effects between any dose of Eletriptan and placebo. The incidence of minor adverse effects was significantly higher for all Eletriptan doses than for placebo, with NNHs of 11 (95% confidence interval, 6.2 to 39), 7.0 (5.2 to 11) and 3.7 (3.1 to 4.5) for Eletriptan 20 mg, 40 mg and 80 mg, respectively. Reviewer's conclusions: Eletriptan 20 mg, 40 mg and 80 mg are effective for the treatment of an acute migraine attack. Effectiveness is dose-related, with statistically significant differences between doses for pain-free response and 24-hour outcomes. Eletriptan compares well with other triptans available for outcomes measured up to 2 hours and provides meaningful relief for 24 hours. Taken as a single dose, Eletriptan was well tolerated and caused no major harm. The incidence of minor harm was dose-dependent, with 80 mg giving significantly more adverse effects than 40 mg.