Ketanserin (tartrate)

Ketanserin is a potent antagonist of the serotonin (5-HT) receptor that is selective for 5-HT₂ (IC₅₀ = 6.3 nM; K_i = 2.1 nM).¹ It has no activity at 5-HT₁ receptors but does have activity at histamine type 1, α₁-adrenergic, and dopamine receptors with K_i values of 10, 10, and 220 nM, respectively. Ketanserin induces dose-dependent inhibition of contractile responses to 5-HT in isolated rat caudal artery, canine basilar, carotid, coronary and gastrosplenic arteries, and canine gastrosplenic and saphenous veins.² Ketanserin (10 mg/kg/day) significantly decreases blood pressure (BP), blood pressure variability (BPV), and hypertensive organ damage in spontaneously hypertensive rats.³ Formulations containing ketanserin have been used to treat hypertension in early-onset preeclampsia.⁴

WARNING This product is not for human or veterinary use.

1. Leysen, J.E., Awouters, F., Kennis, L., et al. Receptor binding profile of R 41 468, a novel antagonist at 5-HT₂ receptors. Life Sci. 28(9), 1015-1022 (1981).

2. Van Neuten, J.M., Janssen, P.A.J., Van Beek, J., et al. Vascular effects of ketanserin (R 41 468), a novel antagonist of 5-HT₂ serotonergic receptors. J. Pharmacol. Exp. Ther. 218(1), 217-230 (1981).

3. Du, W.-M., Miao, C.-Y., Liu, J.-G., et al. Effects of long-term treatment with ketanserin on blood pressure variability and end-organ damage in spontaneously hypertensive rats. J. Cardiovasc. Pharmacol. 41(2), 233-239 (2003).

4. Bijvank, S.W.N., Visser, Q., Duvekot, J.J., et al. Ketanserin versus dihydralazine for the treatment of severe hypertension in early-onset preeclampsia: a double blind randomized controlled trial. Eur. J. Obstet. Gynecol. Reprod. Biol. 189, 106-111 (2015).