Volinanserin
Based on 10 publication(s) in Google Scholar
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.
- Purity: 99.62%
- CAS No.: 139290-65-6
- Formula: C22H28FNO3
- Molecular Weight:373.46
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Publications Citing Use of MedChemExpress (MCE) Volinanserin
More- Br J Pharmacol. 2026 Feb 27. [Abstract]
- Biomed Pharmacother. 2025 Nov 11:193:118742. [Abstract]
- Eur J Pharmacol. 2025 Nov 5:1006:178170. [Abstract]
- Eur J Pharmacol. 2024 Apr 15:969:176466. [Abstract]
- Neuropharmacology. 2025 Dec 23:286:110815. [Abstract]
- Ultrasonics. 2023 Dec:135:107132. [Abstract]
- Psychopharmacology (Berl). 2023 Jun;240(6):1275-1285. [Abstract]
- Addict Biol. 2020 May 26;e12926. [Abstract]
- Behav Brain Res. 2023 Feb 2:437:114127. [Abstract]
- Authorea. September 19, 2022.
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All 5-HT Receptor Isoforms
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Biological Activity
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5-HT1C Receptor |
5-HT2 Receptor 0.36 nM (Ki) |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 139290-65-6
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Appearance Solid
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Molecular Weight 373.46
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Formula C22H28FNO3
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Color White to yellow
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SMILES
FC1=CC=C(CCN2CCC([C@@]([H])(O)C3=CC=CC(OC)=C3OC)CC2)C=C1
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Synonyms
MDL100907; M 100907
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (10)
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Journal Impact Factor
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Most Recent
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Br J Pharmacol
5-HT2A receptors in the prelimbic cortex VIP-expressing interneurons: A mechanism for psychedelic-induced innate fear attenuation. [Abstract]2026 Feb 27. PMID: 41761564 -
Biomed Pharmacother
Ibogalogs improve spatial and recognition memory in rodents through a mechanism involving 5-HT2A receptor activation-enhanced NMDA receptor activity in hippocampal pyramidal CA1 neurons. [Abstract]2025 Nov 11:193:118742. PMID: 41223759
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.
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Eur J Pharmacol
2,5-Dimethoxy-4-methylamphetamine (DOM)-induced gait alterations in mice: Dissecting the role of 5-HT2A/2C receptor-mediated mechanisms. [Abstract]2025 Nov 5:1006:178170. PMID: 40962017 -
Eur J Pharmacol
The psychomotor, reinforcing, and discriminative stimulus effects of synthetic cathinone mexedrone in male mice and rats. [Abstract]2024 Apr 15:969:176466. PMID: 38431243
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.
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Neuropharmacology
Dorsal raphe serotonergic neurons facilitate arousal from sevoflurane anesthesia by heterogeneously modulating neuronal activity in the basolateral amygdala. [Abstract]2025 Dec 23:286:110815. PMID: 41448357 -
Ultrasonics
Transcranial ultrasound neuromodulation facilitates isoflurane-induced general anesthesia recovery and improves cognition in mice. [Abstract]2023 Dec:135:107132. PMID: 37604030 -
Psychopharmacology (Berl)
The effects of serotonergic psychedelics in synaptic and intrinsic properties of neurons in layer II/III of the orbitofrontal cortex. [Abstract]2023 Jun;240(6):1275-1285. PMID: 37071130 -
Addict Biol
Effects of 5-HT2A receptor stimulation on economic demand for fentanyl after intermittent and continuous access self-administration in male rats. [Abstract]2020 May 26;e12926. PMID: 32458577
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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Behav Brain Res
TCB-2, a 5-hydroxytryptamine 2A receptor agonist, disrupts prepulse inhibition in the ventral pallidum and nucleus accumbens. [Abstract]2023 Feb 2:437:114127. PMID: 36174843 -
Solvent & Solubility
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)
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.
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.
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 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.
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.
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.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (537 KB)
- English - EN (537 KB)
- Français - FR (537 KB)
- Deutsch - DE (537 KB)
- Norwegian - NO (537 KB)
- Español - ES (537 KB)
- Swedish - SV (537 KB)
- Italian - IT (537 KB)
- Korean - KR (537 KB)
- Portuguese - PT (537 KB)
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Handling Instructions (2659 KB)
References
[1]. Sorensen SM, et al. Characterization of the 5-HT2 receptor antagonist MDL 100907 as a putative atypical antipsychotic: behavioral, electrophysiological and neurochemical studies. J Pharmacol Exp Ther. 1993 Aug;266(2):684-91. [Content Brief]
[2]. Ardayfio PA, et al. The 5-hydroxytryptamine2A receptor antagonist R-(+)-alpha-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl-4-piperidinemethanol (M100907) attenuates impulsivity after both drug-induced disruption (dizocilpine) and enhancement (antidepressant drugs) of differential-reinforcement-of-low-rate 72-s behavior in the rat. J Pharmacol Exp Ther. 2008 Dec;327(3):891-7. [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, 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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