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      Sumatriptan Succinate (GR43175)
      Sumatriptan Succinate (GR43175)

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      This product is for research use only, not for human use. We do not sell to patients.
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      InvivoChem Cat #: V0988
      CAS #: 103628-48-4Purity ≥98%

      Description: Sumatriptan Succinate (GR-43175; GR43175; Sumatran; Sumax), an approved triptan sulfa drug and a sulfonamide compound, is a selective 5-HT1 receptor agonist used for the treatment of migraine headaches. It has specificity for 5-HT1D, 5-HT1B and 5-HT1A. Sumatriptan Succinate is the succinate salt of sumatriptan.

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

      Related CAS #: 103628-48-4 (succinate); 103628-46-2 (free); 143675-45-0 (hemisulfate) 

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      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


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      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. 
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      References

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

      These protocols are for reference only. InvivoChem does not independently validate these methods.

       
      Sumatriptan Succinate
      Time-course curves of the effects of various doses of sumatriptan or saline on the mechanical response thresholds in the infraorbital nerve territory ipsilateral and contralateral to the ligature. Br J Pharmacol. 2002 Dec;137(8):1287-97.
      		 
      Sumatriptan Succinate
      Br J Pharmacol. 2002 Dec;137(8):1287-97.

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