Rizatriptan-d6 is intended for use as an internal standard for the quantification of rizatriptan by GC- or LC-MS. Rizatriptan is an agonist of the serotonin (5-HT) receptor subtypes 5-HT1B and 5-HT1D (Kis = 4.3 and 10.1 nM, respectively).1 It is selective for 5-HT1B and 5-HT1D receptors over 5-HT1A receptors (Ki = 140 nM). Rizatriptan induces vasoconstriction in isolated human middle meningeal arteries (EC50 = 90 nM).2 In vivo, rizatriptan (50 and 75 mg/kg) reduces head grooming, the number of oculotemporal strokes, eye blinking, and one-eye closures in a Cacna1a mutant transgenic mouse model of migraine.3 Formulations containing rizatriptan have been used in the treatment of migraine.
1.Xu, Y.-C., Schaus, J.M., Walker, C., et al.N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonistJ. Med. Chem.42(3)526-531(1999) 2.Longmore, J., Razzaque, Z., Shaw, D., et al.Comparison of the vasoconstrictor effects of rizatriptan and sumatriptan in human isolated cranial arteries: Immunohistological demonstration of the involvement of 5-HT1B-receptorsBr. J. Clin. Pharmacol.46(6)577-582(1998) 3.Chanda, M.L., Tuttle, A.H., Baran, I., et al.Behavioral evidence for photophobia and stress-related ipsilateral head pain in transgenic Cacna1a mutant micePain154(8)1254-1262(2013)