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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).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $35 | In Stock | |
5 mg | $51 | In Stock | |
10 mg | $74 | In Stock | |
25 mg | $118 | In Stock | |
50 mg | $178 | In Stock | |
100 mg | $263 | In Stock | |
200 mg | $388 | In Stock | |
1 mL x 10 mM (in DMSO) | $56 | In Stock |
Description | 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). |
Targets&IC50 | 5-HT2 receptor:0.37 nM (ki), D4 receptor:2.93 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]. |
Alias | RP 62203 |
Molecular Weight | 425.52 |
Formula | C23H24FN3O2S |
Cas No. | 127625-29-0 |
Smiles | Fc1ccc(cc1)N1CCN(CCCN2c3cccc4cccc(c34)S2(=O)=O)CC1 |
Relative Density. | 1.331g/cm3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 95 mg/mL (223.26 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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