Ketanserin

Ketanserin is a selective 5-HT2 receptor antagonist. Ketanserin also blocks hERG current (I_hERG) in a concentration-dependent manner (IC₅₀=0.11 μM). IC50 & Target: IC50: 0.11 μM (hERG current)^[1]
IC50: 152±23 μM (5-HT receptor)^[2] In Vitro: Ketanserin at 0.3 μM inhibits the voltage-dependent step current (I_hERG.step) and tail current (I_hERG.tail) of hERG channels with a 5-min exposure^[1]. The synergistic effect observed for AA with 5-HT is, also, blocked by the 5-HT receptor blockers cyproheptadine (IC₅₀=22.0±7 μM), Ketanserin (IC₅₀=152±23 μM). Ketanserin (50-350 μM) inhibits the synergism by blocking the receptor in a dose-dependent manner. The IC₅₀ value of Cyproheptadine is 22±7 μM and Ketanserin is 152±23 μM^[2]. Ketanserin inhibits platelet aggregation with an IC₅₀ of 240 (169-339) nM^[3]. In Vivo: Ketanserin is a 5-HT2A receptor antagonist. Ketanserin significantly reduces BDNF protein levels in numerous brain regions (CA1 and CA3 of the hippocampus, prefrontal cortex, central amygdaloid nucleus, dorsomedial hypothalamic nucleus, dentate gyrus, shell of the nucleus accumbens and midbrain periaqueductal gray). 5-HT_2A antagonist Ketanserin can significantly reduce BDNF mRNA levels in various brain regions^[4].