Donitriptan (hydrochloride)

Donitriptan is an agonist of the serotonin (5-HT) receptor subtypes 5-HT_1B and 5-HT_1D.¹ It inhibits forskolin-induced cAMP formation in C6 cells expressing the human receptors (pD₂ = 8.91 and 9.57, respectively). Donitriptan is selective for 5-HT_1B and 5-HT_1D (K_is = 0.36 and 0.15 nM, respectively, for the human receptors) over 5-HT_1A, 5-HT_1E, and 5-HT_1F (K_is = 25, 1,148, and 3,388 nM, respectively) and 5-HT_2A, 5-HT_5A, 5-HT₆, and 5-HT₇ (K_is = 182, 813, 2,344, and 371 nM, respectively). It induces contractions in rabbit saphenous vein rings (pD₂ = 7.1) and increases outward steady-state hyperpolarizing potassium currents (I_K) in isolated guinea pig trigeminal ganglion cells when used at a concentration of 100 nM. In vivo, donitriptan (0.63 and 2.5 mg/kg) decreases total carotid blood flow and increases vascular resistance but does not affect mean arterial pressure or heart rate in anesthetized pigs.

WARNING This product is not for human or veterinary use.

1. John, G.W., Pauwels, P.J., Perez, M., et al. F 11356, a novel 5-hydroxytryptamine (5-HT) derivative with potent, selective, and unique high intrinsic activity at 5-HT_1B/1D receptors in models relevant to migraine. J. Pharmacol. Exp. Ther. 290(1), 83-95 (1999).