83846-83-7

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). 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. Ketanserin (10 mg/kg/day) significantly decreases blood pressure (BP), blood pressure variability (BPV), and hypertensive organ damage in spontaneously hypertensive rats. Formulations containing ketanserin have been used to treat hypertension in early-onset preeclampsia.

coccidiostat

Selective 5-HT2A serotonin receptor antagonist

Selective 5-HT 2A serotonin receptor antagonist; can also be used to discriminate between 5-HT 1D and 5-HT 1B receptor subtypes.

Selective 5-HT2 serotonin receptor antagonist. Ketanserin significantly reduces nicotine self-administration in rats, supporting an unexpected involvement of serotonin in nicotine addiction.

Room temperature

[1] J.E. LEYSEN. Receptor binding profile of R 41 468, A novel antagonist at 5-HT2 receptors[J]. Life sciences, 1981, 28 9: Pages 1015-1022. DOI: 10.1016/0024-3205(81)90747-5
[2] J M VAN NUETEN. Vascular effects of ketanserin (R 41 468), a novel antagonist of 5-HT2 serotonergic receptors.[J]. Journal of Pharmacology and Experimental Therapeutics, 1981, 218 1: 217-230.
[3] WEN-MIN DU. Effects of long-term treatment with ketanserin on blood pressure variability and end-organ damage in spontaneously hypertensive rats.[J]. Journal of Cardiovascular Pharmacology, 2003, 41 2: 233-239. DOI: 10.1097/00005344-200302000-00012
[4] SEBASTIAAN W. NIJ BIJVANK . Ketanserin versus dihydralazine for the treatment of severe hypertension in early-onset preeclampsia: a double blind randomized controlled trial[J]. European journal of obstetrics, gynecology, and reproductive biology, 2015, 189: Pages 106-111. DOI: 10.1016/j.ejogrb.2015.02.002