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Technical Data
| Formula | C14H21N3O2S·C4H6O4 |
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| Molecular Weight | 413.49 | CAS No. | 103628-48-4 | |
| Solubility (25°C)* | In vitro | DMSO | 83 mg/mL (200.73 mM) | |
| Water | 83 mg/mL (200.73 mM) | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | Sumatriptan Succinate (GR 43175) is a triptan sulfa drug containing a sulfonamide group for the treatment of migraine headaches. | |
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| In vitro | Sumatriptan displays the highest affinity for 5-HT1D (Ki = 17 nM) and 5-HT1B (Ki = 27 nM) binding sites and is slightly less potent at 5-HT1A binding sites (Ki = 100 nM). [1] Sumatriptan markedly attenuates plasma protein extravasation induced by electrical trigeminal ganglion stimulation. Sumatriptan reduces morphological changes in post-capillary venules and mast cells within dura mater following electrical trigeminal ganglion stimulation. [2] | |
| In vivo | Sumatriptan at a clinically relevant dose (100 mg/kg, s.c.) leads to a significant reduction of the mechanical allodynia-like behaviour on both the injured and the contralateral sides (peak-effects 6.3 g and 4.4 g, respectively) in a rat model of trigeminal neuropathic pain. [3] Sumatriptan reduces the numbers of Fos-positive cells found in laminae I and IIo of the trigeminal nucleus caudalis and C2 (6, 13 cells and 9 cells, respectively) after mechanical stimulation in cats. [4] Sumatriptan constricts selectively the cranial vessels that are distended and inflamed during migraine, the action is mediated by activation of a 5-HT1 receptor subtype which has been shown in animals to be localized in cranial vessels. Sumatriptan results in oral bioavailabilities of 37, 58 and 23% in rat, dog and rabbit, respectively. sumatriptan is cleared rapidly by metabolic and renal clearance with a half-life of 1-2 hour in rat, dog and rabbit. Sumatriptan produces few adverse pharmacodynamic effects when administered acutely, except at high doses, although it is less well tolerated in dogs. [5] |
Protocol (from reference)
References
Selleck's Sumatriptan Succinate has been cited by 1 publication
| Evaluation system for arrhythmogenic potential of drugs using human-induced pluripotent stem cell-derived cardiomyocytes and gene expression analysis. [Higa A, et al. J Toxicol Sci, 2017, 42(6):755-761] | PubMed: 29142174 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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