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.
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- Pureza : 99.62%
- No. CAS: 139290-65-6
- Fòrmula: C22H28FNO3
- Peso molecular:373.46
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) Volinanserin
More- Br J Pharmacol. 2026 Feb 27. [Abstract]
- Eur J Pharmacol. 2025 Nov 5:1006:178170. [Abstract]
- Eur J Pharmacol. 2024 Apr 15:969:176466. [Abstract]
- Ultrasonics. 2023 Dec:135:107132. [Abstract]
- Neuropharmacology. 2026 Mar 15:286:110815. [Abstract]
- Psychopharmacology (Berl). 2023 Jun;240(6):1275-1285. [Abstract]
- Behav Brain Res. 2023 Feb 2:437:114127. [Abstract]
- Addict Biol. 2021 May;26(3):e12926. [Abstract]
- Biomed Pharmacother. 2025 Dec:193:118742. [Abstract]
- Authorea. September 19, 2022.
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Ver todos los productos específicos de isoformas 5-HT Receptor
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Actividad biológica
Descripciòn
IC50 & Target
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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. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 139290-65-6
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Appearance Solid
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Peso molecular 373.46
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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 -
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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Ultrasonics
Transcranial ultrasound neuromodulation facilitates isoflurane-induced general anesthesia recovery and improves cognition in mice. [Abstract]2023 Dec:135:107132. PMID: 37604030 -
Neuropharmacology
Dorsal raphe serotonergic neurons facilitate arousal from sevoflurane anesthesia by heterogeneously modulating neuronal activity in the basolateral amygdala. [Abstract]2026 Mar 15:286:110815. PMID: 41448357 -
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 -
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 -
Addict Biol
Effects of 5-HT2A receptor stimulation on economic demand for fentanyl after intermittent and continuous access self-administration in male rats. [Abstract]2021 May;26(3):e12926. PMID: 32458577
Volinanserin purchased from MedChemExpress. Usage Cited in: Addict Biol. 2021 May;26(3):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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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 Dec:193:118742. PMID: 41223759
Volinanserin purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2025 Dec: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 Dec: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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Solvente y solubilidad
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)
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)
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.
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.
In Vivo Dissolution Calculator
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.
Pureza y Documentación
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Ficha de datos (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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Instrucciones de manejo (2659 KB)
Referencias
[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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