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Sumatriptan Succinate(GR43175)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Sumatriptan Succinate(GR43175)图片
CAS NO:103628-48-4
规格:≥98%
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
2g电议
5g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)413.49
FormulaC14H21N3O2S·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)
Other info

Chemical Name: 1-(3-(2-(dimethylamino)ethyl)-1H-indol-5-yl)-N-methylmethanesulfonamide succinate

SMILES Code: O=S(CC1=CC2=C(NC=C2CCN(C)C)C=C1)(NC)=O.O=C(O)CCC(O)=O

SynonymsGR 43175; Sumatriptan; GR-43175; GR43175; Sumatran; Sumax
实验参考方法
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.

In VivoSumatriptan 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.
Animal model
Formulation & Dosage
References

Eur J Pharmacol. 1989 Apr 12;163(1):133-6; Br J Pharmacol. 2002 Dec;137(8):1287-97.