Fananserin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Fananserin 是一种有效的、选择性的、口服活性的 5-HT2 拮抗剂（对于大鼠 5-HT2A，Ki = 0.37 nM）。

Fananserin is an effective, selective and oral active antagonist of 5-HT2 (Ki = 0.37 nM for the rat 5-HT2A). Fananserin is an antagonist of human D4 receptor (Ki = 2.93 nM).(In Vitro):Fananserin displays low to moderate affinity for α1-adrenoceptors, dopamine D2 receptors and histamine H 1 receptors. Fananserin displaces [3H]spiperone binding to recombinant human dopamine D 4 receptors with a Ki of 2.93 nM. Fananserin is relatively selective for 5-HT2 receptor with lower affinity for the 5-HT1A receptor and very low affinity for the 5-HT3 receptor.(In Vivo):Fananserin shows a moderate affinity for alpha 1-adrenoceptors in the rat thalamus with an IC50 of 14 nM and for H1 receptors in the guinea-pig cerebellum with an IC50 of 13 nM. Fananserin displaces [125I]AMIK from 5-HT2 receptors with an IC50 of 0.21 nM in the rat frontal cortex. Fananserin (0.5, 1, 2 and 4 mg/kg; p.o.) dose-dependently increases the duration of deep nonrapid eye movement (NREM) sleep at the expense of wakefulness.

Fananserin is relatively selective for 5-HT2 receptor, having lower affinity for the 5-HT1A receptor and very low affinity for the 5-HT3 receptor.Fananserin displaces [3H]spiperone binding to recombinant human dopamine D 4 receptors with a Ki of 2.93 nM.RP 62203 displays low to moderate affinity for α1-adrenoceptors, dopamine D2 receptors and histamine H 1receptors.

Fananserin displaces [125I]AMIK from 5-HT2 receptors with an IC50 of 0.21 nM in rat frontal cortex.Fananserin shows moderate affinity for alpha 1-adrenoceptors in the rat thalamus (IC50 = 14 nM) and for histamine H1 receptors in the guinea-pig cerebellum (IC50 = 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.

RP 62203

GPCR/G Protein

Dopamine Receptor

D2

——

——

127625-29-0

425.52

C23H24FN3O2S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (235.01 mM)

Fc1ccc(cc1)N1CCN(CCCN2c3cccc4cccc(c34)S2(=O)=O)CC1

——

(-20℃)

With Ice Pack

≥ 2 years