Eletriptan-d3 (hydrobromide)

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. 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). Formulations containing eletriptan have been used in the treatment of migraine headache.