| Name | Sumatriptan succinate |
| Description | Sumatriptan succinate (GR 43175), a serotonin1 (5-HT1) receptor agonist, is used in the acute treatment of a migraine headache. |
| In vitro | Sumatriptan is rapidly cleared through metabolism and renal elimination, with a half-life of 1-2 hours. It rarely produces adverse effects when administered acutely, except for dogs exhibiting low tolerance to high doses. Clinically, subcutaneous injection of Sumatriptan at 100 mg/kg notably decreases injury-induced and contralateral mechanical allodynia in a rat model of trigeminal neuropathic pain (peak effects at 6.3g and 4.4g, respectively). In cats, Sumatriptan reduces the number of Fos-positive cells in the caudal part of the spinal trigeminal nucleus (I, IIO, and C2) following mechanical stimulation (to 6, 13, and 9 cells, respectively). The compound's biological activity varies across species, with 37%, 23%, and 58% in rats, rabbits, and dogs, respectively. Sumatriptan selectively constricts cranial blood vessels, which are dilated and inflamed during migraines, mediated by the 5-HT1 receptor subtype in animal cranial vasculature. |
| In vivo | Sumatriptan significantly reduces plasma protein-induced extravasation triggered by electrical stimulation of the trigeminal nerve. It mitigates morphological changes in the capillaries within the dura mater and small veins in the presence of hypertrophied mast cells stimulated at the trigeminal ganglion. Sumatriptan has a slightly lower affinity for the serotonin receptor 1A binding site (KI=100 nM), while exhibiting the highest affinity for 5HT (Ki=17 nM) and 5HT1B receptor binding sites (Ki=27 nM). |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 55 mg/mL (133.01 mM), Sonication is recommended.
H2O : 41.4 mg/mL (100.12 mM), Sonication is recommended.
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| Keywords | Sumatriptan succinate | Sumatriptan Succinate | Sumatriptan | Serotonin Receptor | orally active | migraine headache | Inhibitor | inhibit | GR-43175 | GR43175 | antimigraine activity | 5-hydroxytryptamine Receptor | 5HTReceptor | 5-HT1D | 5-HT1B | 5-HT Receptor | 5HT Receptor | 5-HT |
| Inhibitors Related | Alverine citrate | Olanzapine | Dapoxetine hydrochloride | Clozapine N-Oxide | Mirtazapine | D-Menthol | Amitriptyline hydrochloride | Cloperastine hydrochloride | Trazodone hydrochloride | Mianserin hydrochloride | Fluoxetine hydrochloride | Cinchonidine |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Pain-Related Compound Library | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
