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

Volinanserin  (Synonyms: MDL100907; M 100907)

Cat. No.: HY-14940 Purity: 99.76%
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Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity.

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

Volinanserin Chemical Structure

Volinanserin Chemical Structure

CAS No. : 139290-65-6

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10 mM * 1 mL in DMSO
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Based on 6 publication(s) in Google Scholar

Other Forms of Volinanserin:

Volinanserin Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

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Description

Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity.

IC50 & Target

5-HT2 Receptor

0.36 nM (Ki)

In Vitro

Volinanserin (MDL 100907) is a potent antagonist at the 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c receptor, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Volinanserin Related Antibodies
In Vivo

Volinanserin (MDL 100907; 0.008-2.0 mg/kg, i.p.) significantly decreases d-amphetamine-stimulated locomotor activity in mice, with an ED50 of 0.3 mg/kg, but shows no obvious reduction in the base-line locomotor activity in mice. Volinanserin produces atalepsy with an ED50 of 10-50 mg/kg in rats. Volinanserin does not reduces apomorphine-induced stereotypies or produces catalepsy in rats[1]. Volinanserin (M100907) combined with MK-801 significantly decreases reinforcers at 1 μg/kg, but dose-dependently (10, 100 μg/kg) antagonizes the disruptive effect of MK-801 in rats via i.p. administration. Volinanserin (6.25 μg/kg) enhances the antidepressant-like action of desipramine in rats performing under a DRL 72-s schedule, and elevates the antidepressant-like effect of tranylcypromine[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

373.46

Formula

C22H28FNO3
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

FC1=CC=C(CCN2CCC([C@@]([H])(O)C3=CC=CC(OC)=C3OC)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 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (133.88 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 2.6777 mL 13.3883 mL 26.7766 mL
5 mM 0.5355 mL 2.6777 mL 5.3553 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • Molarity Calculator

  • 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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.
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: 99.76%

COA (247 KB) HNMR (272 KB) LCMS (258 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[1]

Mice[1]
To measure the effects the test compounds alone on spontaneous locomotor activity, mice are injected i.p. with the test compounds, placed singly into clear Plexiglas test cages (16 × 16 × 8 inches) and are allowed to acclimatize for 30 mm. Six mice per dose for each of the six doses are tested for Volinanserin (0.008-2.0 mg/kg), amperozide and haloperidol. Twelve mice per dose for six doses are tested for clozapine. Sixty animals are given vehicle in these experiments. Thereafter, the boxes are placed in the activity monitors and measurements are taken for 30 mm. To measure the effects of various pretreatments on amphetamine stimulated motor activity, mice (four per test box) are acclimatized for 90 mm to reduce the level of spontaneous activity of the controls. The mice are then injected with amphetamine (2 mg/kg i.p.) as well as the test compounds, returned to the activity boxes and tested for 90 mm. In these experiments 16 mice per dose are tested for the 9 doses of Volinanserin and 16 mice per dose are tested for each of 6 doses for amperozide, clozapine and haloperidol. One hundred forty four mice received vehicle in these experiments[1].
Rats[1]
Drugs and doses used are clozapine (1, 10 and 50 mg/kg) or Volinanserin (1, 10 and 50 mg/kg), amperozide (1, 10 and 50 mg/kg) and haloperidol (0.1, 0.3 and 1.0 mg/kg). Five rats per dose are used in these experiments and five rats receive vehicle. Rats are dosed i.p. and, 30 mm later, each rat is placed gently into a clear Plexiglas enclosure (30 × 30 × 15 cm) so that both front limbs rested on top of a horizontal aluminum rod (1.2 cm in diameter). The rod is centered across the plastic enclosure at a height of 7 cm above the floor. The time each rat remained with its hind legs on the floor while the front limbs are elevated on the rod is recorded to the nearest second. Data are analyzed by using analysis of variance followed by appropriate post-hoc tests[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6777 mL 13.3883 mL 26.7766 mL 66.9416 mL
5 mM 0.5355 mL 2.6777 mL 5.3553 mL 13.3883 mL
10 mM 0.2678 mL 1.3388 mL 2.6777 mL 6.6942 mL
15 mM 0.1785 mL 0.8926 mL 1.7851 mL 4.4628 mL
20 mM 0.1339 mL 0.6694 mL 1.3388 mL 3.3471 mL
25 mM 0.1071 mL 0.5355 mL 1.0711 mL 2.6777 mL
30 mM 0.0893 mL 0.4463 mL 0.8926 mL 2.2314 mL
40 mM 0.0669 mL 0.3347 mL 0.6694 mL 1.6735 mL
50 mM 0.0536 mL 0.2678 mL 0.5355 mL 1.3388 mL
60 mM 0.0446 mL 0.2231 mL 0.4463 mL 1.1157 mL
80 mM 0.0335 mL 0.1674 mL 0.3347 mL 0.8368 mL
100 mM 0.0268 mL 0.1339 mL 0.2678 mL 0.6694 mL
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Volinanserin 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:

Volinanserin139290-65-6MDL100907 M 100907MDL 100907MDL-100907M100907M 100907M-1009075-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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