product name Sumatriptan Succinate
Description: Sumatriptan Succinate (also known as GR 43175) is a triptan sulfa drug containing a sulfonamide group for the treatment of migraine headaches. Sumatriptan succinate is a selective 5-HT1 receptor agonist with specificity towards 5-HT1D, 5-HT1B and 5-HT1A. In addition, the physicochemical properties of Sumatriptan succinate can be characterized using FT-IR, HPLC, SEM and XRD. 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).
References: Eur J Pharmacol. 1989 Apr 12;163(1):133-6; Br J Pharmacol. 2002 Dec;137(8):1287-97.
413.49
Formula
C14H21N3O2S·C4H6O4
CAS No.
103628-48-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 83 mg/mL (200.7 mM)
Water: <1 mg/mL
Ethanol: 83 mg/mL (200.7 mM)
Solubility (In vivo)
Synonyms
GR 43175
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
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| Formulation & Dosage | |
| References | Eur J Pharmacol. 1989 Apr 12;163(1):133-6; Br J Pharmacol. 2002 Dec;137(8):1287-97. |
