Catalog No.S1432 Synonyms: GR 43175
Molecular Weight(MW): 413.49
Sumatriptan Succinate is a triptan sulfa drug containing a sulfonamide group for the treatment of migraine headaches.
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|Description||Sumatriptan Succinate is a triptan sulfa drug containing a sulfonamide group for the treatment of migraine headaches.|
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).  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. 
|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.  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.  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. |
-  Peroutka SJ, et al. Eur J Pharmacol, 1989, 163(1), 133-136.
-  Buzzi MG, et al. Cephalalgia, 1991, 11(4), 165-168.
-  Kayser V, et al. Br J Pharmacol, 2002, 137(8), 1287-1297.
|In vitro||DMSO||83 mg/mL (200.73 mM)|
|Water||83 mg/mL (200.73 mM)|
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