法南色林

生物活性靶点体外研究体内研究法南色林试剂级价格

法南色林

CAS号:127625-29-0
英文名:Fananserin
中文名:法南色林
CBNumber:CB71073778
分子式:C23H24FN3O2S
分子量:425.52
MOL File:127625-29-0.mol

法南色林化学性质

熔点 :95-97 °C(Solv: acetonitrile (75-05-8))
沸点 :641.1±65.0 °C(Predicted)
密度 :1.331±0.06 g/cm3(Predicted)
储存条件 :Store at RT
溶解度 :Soluble to 100 mM in DMSO
形态 :Powder
酸度系数(pKa) :7.31±0.10(Predicted)

法南色林性质、用途与生产工艺

生物活性 Fananserin (RP 62203) 是一种口服生物可利用，高效、选择性的 5- 羟色胺 (5-HT2) 受体拮抗剂，对大鼠 5-HT2 受体作用的 Ki 值为 0.37 nM。Fananserin也是一种选择性的多巴胺 D4 受体拮抗剂，对人多巴胺 D4 受体作用的 Ki 值为 2.93 nM。
靶点

5-HT ₂ Receptor

0.37 nM (Ki)

D ₄ Receptor

2.93 nM (Ki)
体外研究

Fananserin is relatively selective for 5-HT ₂ receptor, having lower affinity for the 5-HT _1A receptor and very low affinity for the 5-HT ₃ receptor.
Fananserin displaces [ ³ H]spiperone binding to recombinant human dopamine D 4 receptors with a K _i of 2.93 nM.
RP 62203 displays low to moderate affinity for α1-adrenoceptors, dopamine D2 receptors and histamine H ₁ receptors.

体内研究

Fananserin displaces ^[125I] AMIK from 5-HT ₂ receptors with an IC ₅₀ of 0.21 nM in rat frontal cortex.
Fananserin shows moderate affinity for alpha 1-adrenoceptors in the rat thalamus (IC ₅₀ = 14 nM) and for histamine H1 receptors in the guinea-pig cerebellum (IC ₅₀ = 13 nM).
Fananserin (0.5-4 mg/kg; p.o.) increases the duration of deep nonrapid eye movement (NREM) sleep at the expense of wakefulness in a dose-dependent manner.

Animal Model:	Adult male Sprague Dawley rats (250-300 g)
Dosage:	0.5 mg/kg, 1 mg/kg,2 mg/kg, 4 mg/kg
Administration:	Oral administration
Result:	Increased the duration of deep nonrapid eye movement (NREM) sleep at the expense of wakefulness in a dose-dependent manner from 0.5 mg/kg.