almotriptanmaleate
Almotriptan
CAS: 181183-52-8;154323-57-6
Molecular Formula: C21H31N3O7S
almotriptanmaleate - Names and Identifiers
almotriptanmaleate - Physico-chemical Properties
| Molecular Formula | C21H31N3O7S |
| Molar Mass | 469.55 |
| Melting Point | 170-172°C |
| Boling Point | 538.7°C at 760 mmHg |
| Flash Point | 279.6°C |
| Solubility | Basic Alcohol (Very Slightly), DMSO (Slightly), Methanol (Slightly, Heated) |
| Vapor Presure | 1.13E-11mmHg at 25°C |
| Appearance | powder |
| Color | white to beige |
| Storage Condition | 2-8°C |
almotriptanmaleate - Risk and Safety
| HS Code | 2935904000 |
almotriptanmaleate - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.981 ml | 14.905 ml | 29.809 ml |
| 5 mM | 0.596 ml | 2.981 ml | 5.962 ml |
| 10 mM | 0.298 ml | 1.49 ml | 2.981 ml |
| 5 mM | 0.06 ml | 0.298 ml | 0.596 ml |
Last Update：2024-01-02 23:10:35
almotriptanmaleate - Reference Information
| migraine treatment drug | according to triptan is a triptan-like migraine treatment drug developed by Pfizer in the United States. It was first listed in Australia in May 2001, Denmark, Norway, Sweden and Switzerland in the same year, and in the United Kingdom in 2002. It is suitable for acute treatment of migraine with or without aura in adults. Migraine (Migraine) is a common chronic neurovascular disease, which is characterized by recurrent headache, autonomic dysfunction and different combinations of other neurological symptoms. Attacks are often accompanied by many vegetative nervous system symptoms, such as nausea, vomiting, pale complexion, increased heart rate, increased breathing, gastrointestinal dysfunction, etc., and there are often blurred vision, flashes, hemianopia, and hemianosis before headache attacks. Adropsy manifestations such as lateral numbness, speech difficulties, numbness of the hemiplegia or hemiparesis, lasting several minutes or half an hour. triptans are a class of drugs that selectively excite 5-HT receptors. Since 1990, GlaxoSmithKline's Shumoptan was first used to treat migraine, and in 2003, there have been etroptan, etroptan, etrotriptan, and flrotriptan. Six triptan drugs, including triptan, naltretan, rizatriptan and levomitritriptan, are used in clinical practice. The efficacy of etriptan (almotriptan) is the same as that of sumataptan, but it is better tolerated and costs less than that of sumataptan. Elotriptan (eletriptan) is a new first-line triptan treatment drugs, using 40mg of elotriptan in the treatment of migraine, 2h headache remission rate is better than that of sumataptan 100mg, and has a lower recurrence rate. Zolmitritriptan (zolmitriptan) is a fast and effective drug. 5mg zolmitritriptan nasal spray can be quickly absorbed from nasopharynx, which can be detected in plasma 5min after medication. It is used to treat acute migraine for 15min ~ 4h headache reaction is 70%. Frotriptan (frovatriptan) is a new 5-HTlB/ID agonist. Studies have shown that the 24-hour headache relief rate of Frotriptan in the treatment of menstruation-related migraine is 84%. It is believed that it can be used to treat menstruation-related migraine. |
| pharmacological action | this product is an effective vascular selective 5-HT1B and neuronal 5-HT1D receptor agonist. its affinity for 5-HT1D receptor is 6 times higher than that for sumataptan (Imigran, Imitrex) and 3 times higher than that for 5-HT1B. This product also has a high affinity for 5-HT1F receptors. Human 5-HT1B receptor mediates intracranial vasoconstriction. The 5-HT1D receptor is mainly located in the trigeminal nerve terminal presynaptic. Recent studies have shown that 5-HT1B and 5-HT1F receptors are located in the human trigeminal nerve center. Eletriptan may inhibit the release of neuropeptides by activating the above receptors, thereby producing therapeutic effects. This product has moderate affinity for human 5-HT1A, 5-HT2B, 5-HT1E and 5-HT7 receptors, and has no affinity or pharmacological activity for other receptors (β receptor, adenosine A1, dopamine D1, D2, muscarinic and opioid receptors) and calcium channel dihydropyridine binding sites. Animal experiments show that the selectivity of this product to carotid/coronary artery and femoral artery vascular bed is higher than that of sumataptan. In addition, this product can inhibit neuroinflammation in the dura mater of animals. Therefore, this product may exert anti-migraine effect by constricting intracranial blood vessels and inhibiting neuroinflammation. The lipophilicity of this product is stronger than that of sumataptan and other existing triptan drugs, and can penetrate the blood-brain barrier. |
| biological activity | Almotriptan Malate (LAS 31416) is a selective serotonin 1B/1D(5-HT1B/1D) receptor agonist used to treat migraine attacks in adults. |
| Target | Value |
Last Update：2024-04-09 15:16:48
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View History
almotriptanmaleate
486990-41-4
78278-06-5
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N-acetyl-4-{[(E)-(5-methyl-2-thienyl)methylidene]amino}benzenesulfonamide
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1363381-79-6
543687-12-3
2-hydroxyamino-MeIQx
486990-41-4
78278-06-5
N-(4-fluorophenyl)-2-[4-(hydroxyimino)piperidin-1-yl]acetamide
N-acetyl-4-{[(E)-(5-methyl-2-thienyl)methylidene]amino}benzenesulfonamide
N-[4-(biphenyl-4-yl)-5-phenyl-1,3-thiazol-2-yl]-2-methoxybenzamide
1-(4-Iodophenyl)-3-morpholino-5,6-dihydropyridin-2(1H)-one
1363381-79-6
543687-12-3
2-hydroxyamino-MeIQx