127625-29-0
127625-29-0 结构式
基本信息
Fananserin
2-[3-[4-(4-Fluorophenyl)piperazino]propyl]-2H-naphth[1,8-cd]isothiazole 1,1-dioxide
2-[3-[4-(4-Fluorophenyl)-1-piperazinyl]propyl]-2H-naphthyl[1,8-cd]isothiazole-1,1-dioxide
2H-Naphth[1,8-cd]isothiazole, 2-[3-[4-(4-fluorophenyl)-1-piperazinyl]propyl]-, 1,1-dioxide
常见问题列表
|
5-HT 2 Receptor 0.37 nM (Ki) |
D 4 Receptor 2.93 nM (Ki) |
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.
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. |