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Ketanserin 酮色林;凯坦色林;凯他色林;酮舍林;氟哌喹酮

Ketanserin (R41468, Ketanserinum) 是一种特异性的5-HT2A 5-羟色胺受体拮抗剂,作用于大鼠和人5-HT2A,Ki为2.5 nM。

  • 货号:
    TK0470
  • 规格:
    5mg
    10mg
    50mg
    100mg
  • 价格:
    0.00

产品参数

CAS No.74050-98-9
生物活性Ketanserin is a selective 5-HT2 receptor antagonist. Ketanserin also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).
分子式C22H22FN3O3
分子量395.43
运输条件Room temperature in continental US; may vary elsewhere.
溶解性数据DMSO : 16.67 mg/mL (42.16 mM; Need ultrasonic),DMF : 5 mg/mL (12.64 mM; Need ultrasonic)
体内研究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-HT2A antagonist Ketanserin can significantly reduce BDNF mRNA levels in various brain regions.
体外研究Ketanserin at 0.3 μM inhibits the voltage-dependent step current (IhERG.step) and tail current (IhERG.tail) of hERG channels with a 5-min exposure. 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. Ketanserin inhibits platelet aggregation with an IC50 of 240 (169-339) nM.
纯度及产品资料98%