rac-Eletriptan-d3 is intended for use as an internal standard for the quantification of eletriptan by GC- or LC-MS. Eletriptan is an agonist of the serotonin (5-HT) receptor types 5-HT1B and 5-HT1D.1 It inhibits forskolin-induced cAMP accumulation in and induces vasoconstriction of isolated rabbit common carotid artery rings (pD2s = 7.6 and 4.9, respectively), an effect that can be blocked by the 5-HT1B antagonist SB216641 but not the 5-HT1D antagonist BRL15572. Eletriptan preferentially induces constriction of isolated human cerebral over coronary arteries (EC50s = 15.8 and 1,995 nM, respectively).2 Formulations containing eletriptan have been used in the treatment of migraine headache.
1.Akin, D., Onaran, H.O., and Gudal, H.Agonist-directed trafficking explaining the difference between response pattern of naratriptan and sumatriptan in rabbit common carotid arteryBr. J. Pharmacol.136(2)171-176(2002) 2.Edvinsson, L., Uddman, E., Wackenfors, A., et al.Triptan-induced contractile (5-HT1B receptor) responses in human cerebral and coronary arteries: Relationship to clinical effectClin. Sci. (Lond.)109(3)335-342(2005)