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

Volinanserin  (Synonyms: MDL100907; M 100907)

Cat. No.: HY-14940 Purity: 99.62% ee.: 100%
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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.

CAS No. : 139290-65-6

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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Volinanserin:

Volinanserin Related Antibodies

Top Publications Citing Use of Products

    Volinanserin purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2025 Nov 11:193:118742.  [Abstract]

    The selective antagonists volinanserin (0.05 mg/kg; s.c.) (Vol) and SB242084 (0.5 mg/kg; i.p.) (SB) were administered 15 min before each ibogalog. One-way ANOVA and Tukey’s post hoc analysis of the results (mean ± SEM) indicated that ibogalogs significantly reduced the time required to locate the target hole (C1), distance to the target hole (C3), number of incorrect holes explored (C4), and total latency (C5), whereas they significantly increased the search strategy score (C6). The antagonists volinanserin and SB242084 significantly reduced ibogalog’s effects on number of incorrect holes explored (C4), whereas only volinanserin reduced ibogalog’s effect on search strategy score (C6).

    Volinanserin purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2025 Nov 11:193:118742.  [Abstract]

    Effects of TBG, DM506, and volinanserin (Vol) (0.4 µM) on hippocampal theta rhythm obtained from anesthetized rats. Effects of TBG, DM506, volinanserin, and TBG+Vol on theta rhythm parameters.

    Volinanserin purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2024 Apr 15:969:176466.  [Abstract]

    Representative locomotor tracking pattern (red lines in each gray rectangle) for 60 min after an injection of saline or acute mexedrone with pretreatment of a 5-HT2A receptor antagonist M100907 (Volinanserin, 0.5 or 1.0 mg/kg, s.c.).

    Volinanserin purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2024 Apr 15:969:176466.  [Abstract]

    Effect of M100907 on acute mexedrone-induced locomotor activity (B) and velocity (c) in mice. Data are presented as the mean ± SEM. *P < 0.05 vs. vehicle + saline, #P < 0.05 vs. saline + mexedrone or M100907 (Volinanserin, 0.5 or 1.0 mg/kg, s.c.) + mexedrone. N = 6–7 per group.

    Volinanserin purchased from MedChemExpress. Usage Cited in: Addict Biol. 2020 May 26;e12926.  [Abstract]

    Log2 fold-change in indicated economic demand parameter for each drug condition relative to the log-average of all vehicle sessions. DOI 0.1mg/kg (N=10), 0.2mg/kg (N=10), 0.4 mg/kg (N=7), M100907 + DOI (N=5), M100907 (Volinanserin, 0.3mg/kg, i.p., 50 min prior to testing) alone (N=5).

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    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-HT1C Receptor

     

    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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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:

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    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: 99.62% ee.: 100%

    SDS (537 KB)

    COA (247 KB) HNMR (260 KB) NP-HPLC (139 KB) LCMS (88 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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