Biological Activity
Sumatriptan-d6 is intended for use as an internal standard for the quantification of sumatriptan by GC- or LC-MS. Sumatriptan is an agonist of the serotonin (5-HT) receptor subtypes 5-HT1B and 5-HT1D (IC50s = 9.3 and 7.3 nM, respectively).1 It also binds to the 5-HT1F receptor (IC50 = 17.8 nM). It induces vasoconstriction in isolated human middle meningeal arteries (EC50 = 89.9 nM), an effect that can be reduced by the 5-HT1B/1D receptor antagonists GR125743 and GR127935 . Sumatriptan reduces acute, but not chronic, mechanical hyperalgesia in a mouse model of pain induced by nitroglycerin, which is a known migraine trigger in humans.2 Formulations containing sumatriptan have been used in the treatment of migraine headache.
References
1.Razzaque, Z., Heald, M.A., Pickard, J.D., et al.Vasoconstriction in human isolated middle meningeal arteries: Determining the contribution of 5-HT1B- and 5-HT1F-receptor activationBr. J. Pharmacol.47(1)75-82(1999)
2.Pradhan, A., Smith, M.L., McGuire, B., et al.Characterization of a novel model of chronic migrainePain155(2)269-274(2014)
