Fananserin
Based on 1 Customer Validation
Fananserin (RP 62203) is an orally bioavailable, potent and selective 5-hydroxytryptamine2 (5-HT2) receptor antagonist, with a Ki of 0.37 nM for the rat 5-HT2A receptor. Fananserin also is a selective dopamine D4 receptor antagonist, with a Ki of 2.93 nM for the human dopamine D4 receptor.
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- Pureté: 99.97%
- CAS No.: 127625-29-0
- Formule: C23H24FN3O2S
- Masse moléculaire:425.52
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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5-HT2 Receptor 0.37 nM (Ki) |
5-HT2A Receptor |
D4 Receptor 2.93 nM (Ki) |
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[1].
Fananserin displaces [3H]spiperone binding to recombinant human dopamine D 4 receptors with a Ki of 2.93 nM[1].
RP 62203 displays low to moderate affinity for α1-adrenoceptors, dopamine D2 receptors and histamine H 1 receptors[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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)[2].
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[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male Sprague Dawley rats (250-300 g)[3]
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Dosage:0.5 mg/kg, 1 mg/kg,2 mg/kg, 4 mg/kg
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Administration:Oral administration
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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.
Chemical Information
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CAS No. 127625-29-0
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Appearance Solid
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Masse moléculaire 425.52
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Formule C23H24FN3O2S
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SMILES
FC1=CC=C(N2CCN(CCCN(C3=CC=CC4=C3C5=CC=C4)S5(=O)=O)CC2)C=C1
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Synonyms
RP 62203
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (235.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.88 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Heuillet E, et al. The naphtosultam derivative RP 62203 (fananserin) has high affinity for the dopamine D4 receptor. Eur J Pharmacol. 1996 Oct 24;314(1-2):229-33. [Content Brief]
[2]. Malgouris C, et al. Autoradiographic studies of RP 62203, a potent 5-HT2 receptor antagonist. In vitro and ex vivo selectivity profile. Eur J Pharmacol. 1993 Mar 16;233(1):29-35. [Content Brief]
[3]. Stutzmann JM, et al. RP 62203, a 5-hydroxytryptamine2 antagonist, enhances deep NREM sleep in rats. Sleep. 1992 Apr;15(2):119-24. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3501 mL | 11.7503 mL | 23.5007 mL | 58.7516 mL |
| 5 mM | 0.4700 mL | 2.3501 mL | 4.7001 mL | 11.7503 mL | |
| 10 mM | 0.2350 mL | 1.1750 mL | 2.3501 mL | 5.8752 mL | |
| 15 mM | 0.1567 mL | 0.7834 mL | 1.5667 mL | 3.9168 mL | |
| 20 mM | 0.1175 mL | 0.5875 mL | 1.1750 mL | 2.9376 mL | |
| 25 mM | 0.0940 mL | 0.4700 mL | 0.9400 mL | 2.3501 mL | |
| 30 mM | 0.0783 mL | 0.3917 mL | 0.7834 mL | 1.9584 mL | |
| 40 mM | 0.0588 mL | 0.2938 mL | 0.5875 mL | 1.4688 mL | |
| 50 mM | 0.0470 mL | 0.2350 mL | 0.4700 mL | 1.1750 mL | |
| 60 mM | 0.0392 mL | 0.1958 mL | 0.3917 mL | 0.9792 mL | |
| 80 mM | 0.0294 mL | 0.1469 mL | 0.2938 mL | 0.7344 mL | |
| 100 mM | 0.0235 mL | 0.1175 mL | 0.2350 mL | 0.5875 mL |
Fananserin Related Classifications
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