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). 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.

Selective 5-HT2A serotonin receptor antagonist

coccidiostat

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

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