Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Fananserin is an orally bioavailable and selective antagonist of the 5-HT2 receptor (Ki: 0.37 nM for the rat 5-HT2A receptor). It also is an antagonist of dopamine D4 receptor (Ki: 2.93 nM for the human dopamine D4 receptor).
説明 | Fananserin is an orally bioavailable and selective antagonist of the 5-HT2 receptor (Ki: 0.37 nM for the rat 5-HT2A receptor). It also is an antagonist of dopamine D4 receptor (Ki: 2.93 nM for the human dopamine D4 receptor). |
ターゲット&IC50 | D4 receptor:2.93 nM (ki), 5-HT2 receptor:0.37 nM (ki) |
In vitro | Fananserin displays low to moderate affinity for α1-adrenoceptors, dopamine D2 receptors and histamine H 1 receptors[1]. Fananserin displaces [3H]spiperone binding to recombinant human dopamine D 4 receptors with a Ki of 2.93 nM[3]. 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[3]. |
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[1]. Fananserin displaces [125I]AMIK from 5-HT2 receptors with an IC50 of 0.21 nM in the rat frontal cortex[1]. 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[2]. |
別名 | RP 62203 |
分子量 | 425.52 |
分子式 | C23H24FN3O2S |
CAS No. | 127625-29-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 95 mg/mL (223.26 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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Fananserin 127625-29-0 GPCR/G Protein Neuroscience Dopamine Receptor 5-HT Receptor RP-62203 Inhibitor RP 62203 RP62203 inhibit 5-HT2 dopamine Serotonin Receptor 5-hydroxytryptamine Receptor inhibitor