Size | Price | Stock | Qty |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Fananserin (RP-62203; RP62203) is a novel and potent antipsychotic agent acting as a 5-hydroxytryptamine2 (5-HT2) receptor antagonist (Ki = 0.37 nM for the rat 5-HT2A receptor).
Targets |
5-HT2 Receptor ( Ki = 0.37 nM ); D4 Receptor ( Ki = 2.93 nM )
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ln Vitro |
Fananserin has very little affinity for the 5-HT3 receptor and less affinity for the 5-HT1A receptor, making it comparatively selective for the 5-HT2 receptor[1].
Fananserin displaces [3H]spiperone binding to recombinant human dopamine D 4 receptors with a Ki of 2.93 nM[1].
RP 62203 exhibits low to moderate binding affinity towards histamine H1 receptors, dopamine D2 receptors, and α1-adrenoceptors[2].
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ln Vivo |
Fananserin displaces [125I]AMIK from 5-HT2 receptors at an IC50 of 0.21 nM in rat frontal cortex[2].
Fananserin demonstrates a moderate affinity for the rat thalamus's alpha 1-adrenoceptors (IC50 = 14 nM) and the guinea-pig cerebellum's histamine H1 receptors (IC50 = 13 nM)[2]. Fananserin (0.5-4 mg/kg; p.o.) lengthens the duration of deep nonrapid eye movement (NREM) sleep at the expense of wakefulness in a dose-dependent manner[3]. |
Animal Protocol |
Adult male Sprague Dawley rats (250-300 g)
0.5 mg/kg, 1 mg/kg,2 mg/kg, 4 mg/kg Oral administration |
References |
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Molecular Formula |
C23H24FN3O2S
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Molecular Weight |
425.52
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Exact Mass |
425.16
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Elemental Analysis |
C, 64.92; H, 5.69; F, 4.46; N, 9.88; O, 7.52; S, 7.53
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CAS # |
127625-29-0
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Appearance |
Solid powder
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SMILES |
C1CN(CCN1CCCN2C3=CC=CC4=C3C(=CC=C4)S2(=O)=O)C5=CC=C(C=C5)F
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InChi Key |
VGIGHGMPMUCLIQ-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C23H24FN3O2S/c24-19-8-10-20(11-9-19)26-16-14-25(15-17-26)12-3-13-27-21-6-1-4-18-5-2-7-22(23(18)21)30(27,28)29/h1-2,4-11H,3,12-17H2
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Chemical Name |
3-[3-[4-(4-fluorophenyl)piperazin-1-yl]propyl]-2lambda6-thia-3-azatricyclo[6.3.1.04,12]dodeca-1(11),4,6,8(12),9-pentaene 2,2-dioxide
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Synonyms |
RP-62203; RP 62203; Fananserin; RP62203
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HS Tariff Code |
2934.99.03.00
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~100 mg/mL (~235.0 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.88 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.3501 mL | 11.7503 mL | 23.5007 mL | |
5 mM | 0.4700 mL | 2.3501 mL | 4.7001 mL | |
10 mM | 0.2350 mL | 1.1750 mL | 2.3501 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.