2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor Dopamine Receptor
  4. Fananserin

Fananserin  (Synonyms: RP 62203)

Cat. No.: HY-103104 Purity: 99.97%
COA Handling Instructions

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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.

For research use only. We do not sell to patients.

Fananserin Chemical Structure

Fananserin Chemical Structure

CAS No. : 127625-29-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 116 In-stock
Solution
10 mM * 1 mL in DMSO USD 116 In-stock
Solid
1 mg USD 55 In-stock
5 mg USD 105 In-stock
10 mg USD 150 In-stock
50 mg USD 360 In-stock
100 mg USD 530 In-stock
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Based on 1 publication(s) in Google Scholar

Fananserin Related Antibodies

Top Publications Citing Use of Products

View All 5-HT Receptor Isoform Specific Products:

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

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Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target

5-HT2 Receptor

0.37 nM (Ki)

D4 Receptor

2.93 nM (Ki)

In Vitro

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 Related Antibodies
In Vivo

Fananserin displaces [125I]AMIK from 5-HT2 receptors with an IC50 of 0.21 nM in rat frontal cortex[2].
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.

Animal Model: Adult male Sprague Dawley rats (250-300 g)[3]
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.
Molecular Weight

425.52

Formula

C23H24FN3O2S
CAS No.
Appearance

Solid

SMILES

FC1=CC=C(N2CCN(CCCN(C3=CC=CC4=C3C5=CC=C4)S5(=O)=O)CC2)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.97%

COA (247 KB) HNMR (273 KB) LCMS (269 KB)

Handling Instructions (2659 KB)
References

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
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Fananserin Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Fananserin127625-29-0RP 62203RP62203RP-622035-HT ReceptorDopamine ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT2dopamineD4Inhibitorinhibitorinhibit

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