Isometheptene mucate
(Synonyms: 半乳糖二酸异美汀) 目录号 : GC64514
Isometheptene mucate 是一种拟交感神经剂，是一种间接作用的肾上腺素能受体 (adrenergic receptor) 激动剂。Isometheptene mucate 可用于偏头痛研究。
Cas No.:7492-31-1
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
Isometheptene mucate, a sympathomimetic agent, is a indirect-acting adrenergic receptor agonist. Isometheptene mucate can be used for migraine research[1].
[1]. Alejandro Labastida-RamÍrez, et al. Effects of two isometheptene enantiomers in isolated human blood vessels and rat middle meningeal artery - potential antimigraine efficacy. J Headache Pain. 2019 May 3;20(1):47. https://pubmed.ncbi.nlm.nih.gov/31053059/
| Cas No. | 7492-31-1 | SDF | Download SDF |
| 别名 | 半乳糖二酸异美汀 | ||
| 分子式 | C9H19N.1/2C6H10O8 | 分子量 | 280.77 |
| 溶解度 | 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 | 3.5616 mL | 17.8082 mL | 35.6163 mL |
| 5 mM | 0.7123 mL | 3.5616 mL | 7.1233 mL |
| 10 mM | 0.3562 mL | 1.7808 mL | 3.5616 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。
Comparative study of a combination of Isometheptene mucate, dichloralphenazone with acetaminophen and sumatriptan succinate in the treatment of migraine
Headache 2001 Apr;41(4):391-8.PMID:11318886DOI:10.1046/j.1526-4610.2001.111006391.x.
Objective: To compare the safety and efficacy of Isometheptene mucate, dichloralphenazone with acetaminophen to sumatriptan succinate for the treatment of mild-to-moderate migraine, with or without aura, when taken at the first sign of an attack. Background: The Food and Drug Administration approved sumatriptan succinate and the combination of Isometheptene mucate, dichloralphenazone with acetaminophen for the treatment of migraine. As part of the stratified treatment of migraine, those patients whose headaches are mild or moderate may benefit from nontriptan medications. Additionally, early treatment of acute migraine before the headache has become moderate or severe may improve response to treatment. Methods: This was a multicenter, double-blind, randomized, parallel-group study to assess the safety and efficacy of the combination of Isometheptene mucate, dichloralphenazone with acetaminophen and sumatriptan succinate in the early stages of a single migraine attack. Patients diagnosed with migraine, with or without aura, as defined by the International Headache Society diagnostic criteria were enrolled. Results: One hundred thirty-seven patients were enrolled in the study. Data for efficacy were available for 126 patients; safety data were available for 128 patients. No statistically significant difference between the two active agents in the patient's response to treatment was demonstrated. Headache recurrence was not significantly different over the 24-hour evaluation period for those patients responding in the first 4 hours. In those with headache recurrence, it was statistically significantly more severe in those patients treated with sumatriptan succinate. Improvement in functional disability was, in general, better among those treated with Isometheptene mucate, dichloralphenazone with acetaminophen. Global analysis of efficacy was similar in the two active groups. Patients treated with sumatriptan succinate were somewhat more likely to have adverse effects than the Isometheptene mucate, dichloralphenazone with acetaminophen group. Conclusions: Both Isometheptene mucate, dichloralphenazone with acetaminophen and sumatriptan succinate are safe and effective when used early in the treatment of an acute migraine. Several parameters suggest that Isometheptene mucate, dichloralphenazone with acetaminophen may have a slight advantage compared with sumatriptan succinate in the early treatment of mild-to-moderate migraine.
Life threatening intracerebral hemorrhage with Isometheptene mucate, dichlorophenazine and acetaminophen combination therapy
J Forensic Leg Med 2009 Nov;16(8):489-91.PMID:19782324DOI:10.1016/j.jflm.2009.07.006.
A 45 year old female with no stroke risk factors suffered a massive intracerebral hemorrhage (ICH) after ingesting Midrin--a combination of Isometheptene mucate, dichlorophenazine and acetaminophen. Neuroimaging revealed no evidence of structural disease or underlying vasculopathy. This is the first reported case of isometheptene induced ICH in the absence of underlying cerebrovascular disease. Physicians must be aware of the potential for this complication, and inquire about the use of isometheptene in unexplained cerebral hemorrhages. Neurological communities in countries with nonprescription isometheptene should discourage unsupervised or excessive use of the drug.
Metabolism of isometheptene in human urine and analysis by gas chromatography-mass spectrometry in doping control
J Chromatogr B Analyt Technol Biomed Life Sci 2005 Dec 5;827(2):199-204.PMID:16242387DOI:10.1016/j.jchromb.2005.09.037.
A study of the metabolism of isometheptene, an antispasmodic drug, in man and comparison with heptaminol metabolism, is presented in this paper. Isometheptene and two metabolites were detected in human urine after oral administration of a tablet containing Isometheptene mucate. The urine level of the parent drug, which is excreted during the first 24 h, was determined using gas chromatography-mass spectrometry, after alkaline extraction with organic solvent. A minor metabolite of isometheptene was converted to heptaminol in vitro under the acidic hydrolysis conditions used for the screening procedure of stimulants and narcotics in doping control analysis.
The pharmacology of medications used in treating headache
Semin Pediatr Neurol 1995 Jun;2(2):165-77.PMID:9422244DOI:10.1016/s1071-9091(05)80027-0.
Migraine is a common and disabling disease of uncertain pathogenesis. Research on the trigeminovascular system, serotonin receptors, and substance P have provided clues to improving the pharmacotherapy of this disorder. Selective serotonin agonists, such as sumatriptan, dihydroergotamine, ergotamine tartrate, nonsteroidal anti-inflammatory drugs (NSAIDS), Isometheptene mucate, and phenothiazines are useful to treat acute attacks. Prophylactic agents include beta-blockers, calcium channel blockers, NSAIDs, antidepressants, and valproate. The addition of several new agents for the acute and prophylactic therapy of migraine has improved the outlook for this debilitating disorder.
Classification, mechanisms, and management of headache
Clin Pharm 1984 Mar-Apr;3(2):139-52.PMID:6373100doi
Classification, epidemiology, pathophysiology, and therapy of migraine, cluster, and muscle-contraction (tension) headaches are reviewed. Migraine headache is related to vasomotor changes and is often preceded or accompanied by neurologic symptoms, nausea, and vomiting. Ergot alkaloids are used in acute migraine episodes; products containing caffeine are sometimes used for synergy. Other agents including antiemetic and sedative drugs and a combination product containing Isometheptene mucate , dichloralphenazone , and acetaminophen have been used. Methysergide is the drug of choice for migraine prophylaxis. Of all patients with cluster headache, 90% experience episodes that occur in series separated by intervals as short as one week or as long as 25 years, and the remaining 10% have chronic headache. Pain is unilateral, nausea and vomiting are rare, and there is no aura. Pathophysiology is thought to be similar to that of migraine. Supportive treatment includes drug therapy to improve sleep and avoidance of alcohol and vasodilating agents. Aerosol ergot preparations may be effective for treatment of acute episodes . Prednisone has been used both as an abortive agent and for prophylaxis, while ergotamine, methysergide, and lithium have been tried prophylactically. Chronic tension headache is a constant, tight, pressing, or bandlike sensation in the frontal, temporal, or occipital area that occurs daily. The deep, steady ache differs from the throbbing sensation of vascular headache. Constant overcontraction of scalp muscles may be a cause. Heat, massage, and stretching are used to alleviate excess muscle contraction. Tension headache has been treated with analgesics, nonsteroidal anti-inflammatory agents, muscle relaxants, and amitriptyline. Drug treatment of headache must be based on headache type and tailored to individual response. Bio-feedback may be useful in some patients when combined with drugs.