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Cat. No. Name Size Price Add Cart
KI0756Sumatriptan succinate25 mg$154

Chemical Characteristic

Product NameSumatriptan succinate
SynonymsImitrex, Imigran ,Treximet, GR 43175
CAS No.103628-48-4
Molecular Weight 413.49
FormulaC18H27N3O6S
Chemical Name1-[3-(2-Dimethylaminoethyl)-1H-indol-5-yl]-N-methyl-methanesulfonamide succinate
SmilesC(S(=O)(=O)NC)c1cc2c(c[nH]c2cc1)CCN(C)C C(=O)(CCC(=O)O)O
Chemical Structure

Biological activities

Sumatriptan succinate is the succinate salt form of sumatriptan. Sumatriptan is a selective 5-HT1B/1D-receptor agonist. The IC50 value of sumatriptan for 5-HT1B, 5-HT1D and 5-HT1F receptor is 9.3, 7.3 and 17.8 nM, respectively. The Emax value of sumatriptan for 5-HT1D and 5-HT1B receptor is 98% and 101% of the maximal 5-HT (10 µM), respectively. The Emax value of sumatriptan for HMMA is 105% of the KCl (45 mM).[1]Sumatriptan displays moderate affinity for 5-HT1D and 5-HT1A receptors with Ki of 17 and 100 nM, respectively.[2] Sumatriptan is a full agonist at the h5-HT1B receptor with an IC50 of 20 nM in HEK 293 cells and h5-HT1D receptors with an IC50 of 2.6 nM, respectively.[3] Sumatriptan inhibits evoked IPSCs (inhibitory postsynaptic currents) with an IC50 of 261 nM. Sumatriptan (3 µM) also reduces the amplitude of non-NMDA mediated evoked excitatory postsynaptic currents (EPSCs) in all PAG neurons tested. Sumatriptan inhibits GABAergic and glutamatergic synaptic transmission within the PAG via a 5-HT1B/D receptor mediated reduction in the probability of neurotransmitter release from nerve terminals. Sumatriptan inhibits evoked GABAergic synaptic currents via a presynaptic mechanism.[4] In vitro in rat medullary dorsal horn neurons, sumatriptan inhibits the miniature EPSC (mEPSC) rate in a dose dependent fashion, with an EC50 of 250 nM. Sumatriptan (3 µM) inhibits the mEPSC rate by 36%, without altering the mEPSC amplitude.[5] In rat, local intracortical perfusion with sumatriptan via the dialysis probe decreases cortical 5-HT (5-hydroxytryptamine, serotonin) release with an ED50 value of approximately 0.5 µM.[6] In vivo, sumatriptan (24 and 42 mg/kg) is significantly effective in a reliable animal model of cephalalgia in rats, while having no systemic analgesic activity.[7] In sumatriptan-treated anesthetized pigs, jugular venous oxygen saturation decreases dose dependently with a geometric mean ED50 value of 16 µg/kg, concomitantly with increases in carotid vascular resistance.[8] Sumatriptan reveals selectivity for functional 5-HT1B receptors in rat brain and 5-HT1D receptors in calf brain.[1] Sumatriptan inhibits neurogenic inflammation via 5-HT1Dα receptors in guinea pigs and 5-HT1Dβ (5- HT1B) receptors in rats.[9]

Protocols

In vivo: Sumatriptan is dissolved in saline ( 0.9%).[8]

References

[1] Razzaque Z, et al. Vasoconstriction in human isolated middle meningeal arteries: determining the contribution of 5-HT1B- and 5-HT1F-receptor activation. Br J Clin Pharmacol. 1999, 47(1): 75-82.
[2] McCarthy BG, et al. Comparative neuropharmacology of dihydroergotamine and sumatriptan (GR 43175). Headache. 1989, 29(7): 420-422.
[3] Lesage AS, et al. Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines. Br J Pharmacol. 1998, 123(8): 1655-1665.
[4] Jeong HJ, et al. Sumatriptan inhibits synaptic transmission in the rat midbrain periaqueductal grey. Mol Pain. 2008, 4: 54.
[5] Jennings EA, et al. Effects of sumatriptan on rat medullary dorsal horn neurons. Pain. 2004, 111(1-2): 30-37.
[6] Johnson DE, et al. Serotonergic effects and extracellular brain levels of eletriptan, zolmitriptan and sumatriptan in rat brain. Eur J Pharmacol. 2001, 425(3): 203-210.
[7] Ottani A, et al. Effect of sumatriptan in different models of pain in rats. Eur J Pharmacol. 2004, 497(2): 181-186.
[8] Létienne R, et al. Investigation of the effects of naratriptan, rizatriptan, and sumatriptan on jugular venous oxygen saturation in anesthetized pigs: implications for their mechanism of acute antimigraine action. J Pharmacol Exp Ther. 2003, 307(1): 168-174.
[9] Yu XJ, et al. The 5-HT1D receptor antagonist GR-127,935 prevents inhibitory effects of sumatriptan but not CP-122,288 and 5-CT on neurogenic plasma extravasation within guinea pig dura mater. Neuropharmacology. 1997, 36(1): 83-91.

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