Home Neuronal Signaling 5-HT Receptor agonist Sumatriptan Succinate For research use only.

Sumatriptan Succinate

Synonyms: GR 43175

Sumatriptan Succinate (GR 43175) is a triptan sulfa drug containing a sulfonamide group for the treatment of migraine headaches.

Sumatriptan Succinate Chemical Structure

Sumatriptan Succinate Chemical Structure

CAS No. 103628-48-4

Purity & Quality Control

Sumatriptan Succinate Related Products

Signaling Pathway

5-HT Receptor Signaling Pathways

5-HT Receptor Signaling Pathway

Biological Activity

Description Sumatriptan Succinate (GR 43175) is a triptan sulfa drug containing a sulfonamide group for the treatment of migraine headaches.
Targets
5-HT [1]
In vitro
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
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]

Chemical Information & Solubility

Molecular Weight 413.49 Formula

C14H21N3O2S·C4H6O4
CAS No. 103628-48-4 SDF Download Sumatriptan Succinate SDF
Smiles CNS(=O)(=O)CC1=CC2=C(C=C1)NC=C2CCN(C)C.C(CC(=O)O)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 83 mg/mL ( (200.73 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 83 mg/mL

Ethanol : Insoluble


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In vivo
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