Pimavanserin hemitartrate
Based on 12 publication(s) in Google Scholar
Pimavanserin (ACP-103) hemitartrate is a potent and brain-penetrant5-HT 2A receptor inverse agonist with pIC50 and pKi of 8.73 and 9.3, respectively.
For research use only. We do not sell to patients.
- Purity: 99.91%
- CAS No.: 706782-28-7
- Formula: C25H34FN3O2.1/2C4H6O6
- Molecular Weight:502.59
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
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Publications Citing Use of MedChemExpress (MCE) Pimavanserin hemitartrate
More- Nat Commun. 2023 Dec 15;14(1):8221. [Abstract]
- Proc Natl Acad Sci U S A. 2020 Oct 20;117(42):26438-26447. [Abstract]
- J Med Chem. 2023 Jul 13;66(13):9057-9075. [Abstract]
- Sci Rep. 2024 Jan 16;14(1):1396. [Abstract]
- Int J Neuropsychopharmacol. 2021 Sep 21;24(9):749-757. [Abstract]
- ACS Chem Neurosci. 2019 Nov 20;10(11):4476-4491. [Abstract]
- Food Chem Toxicol. 2023 Jun:176:113800. [Abstract]
- Int J Clin Exp Med. 2019;12(8):10342-10349
- bioRxiv. 2023 Jul 31:2023.07.29.551106. [Abstract]
- Patent. US20200352950A1.
- bioRxiv. 2020 Feb.
- Virginia Commonwealth University. 2016 Oct.
Customer Validation & Images
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
All 5-HT Receptor Isoforms
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Biological Activity
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5-HT2A Receptor 8.73 (pIC50) |
5-HT2A Receptor 9.3 (pKi) |
Pimavanserin hemitartrate competitively antagonizes the binding of [3H]ketanserin to heterologously expressed human 5-HT 2A receptors with a mean pKi of 9.3 in membranes and 9.70 in whole cells. Pimavanserin hemitartrate displays potent inverse agonist activity in the cell-based functional assay receptor selection and amplification technology (R-SAT), with a mean pIC50 of 8.7. Pimavanserin hemitartrate demonstrates lesser affinity (mean pKi of 8.80 in membranes and 8.00 in whole cells, as determined by radioligand binding) and potency as an inverse agonist (mean pIC50 7.1 in R-SAT) at human 5-HT 2C receptors, and lacks affinity and functional activity at 5-HT 2B receptors, dopamine D2 receptors, and other human monoaminergic receptors[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.
Chemical Information
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CAS No. 706782-28-7
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Appearance Solid
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Molecular Weight 502.59
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Formula C25H34FN3O2.1/2C4H6O6
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Color White to off-white
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SMILES
O=C(O)[C@H](O)[C@@H](O)C(O)=O.O=C(NCC1=CC=C(OCC(C)C)C=C1)N(CC2=CC=C(F)C=C2)C3CCN(C)CC3
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Synonyms
ACP-103 hemitartrate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications (12)
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Journal Impact Factor
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Most Recent
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Nat Commun
Identification of 5-HT2A receptor signaling pathways associated with psychedelic potential. [Abstract]2023 Dec 15;14(1):8221. PMID: 38102107 -
Proc Natl Acad Sci U S A
2020 Oct 20;117(42):26438-26447. PMID: 33024014 -
J Med Chem
Design, Synthesis, Molecular Docking, and Biological Evaluation of Novel Pimavanserin-Based Analogues as Potential Serotonin 5-HT2A Receptor Inverse Agonists. [Abstract]2023 Jul 13;66(13):9057-9075. PMID: 37378639
Pimavanserin hemitartrate purchased from MedChemExpress. Usage Cited in: J Med Chem. 2023 Jul 13;66(13):9057-9075. [Abstract]
Compounds 2 and 4 showed similar IC50 values between them and higher potencies than pimavanserin.
Pimavanserin hemitartrate purchased from MedChemExpress. Usage Cited in: J Med Chem. 2023 Jul 13;66(13):9057-9075. [Abstract]
[35S]GTPγS binding values obtained in the presence of pimavanserin, compound 2, compound 3, and compound 4 at 10−5 M in postmortem human prefrontal cortex membrane homogenates both in the absence (plain bars) and in the presence (striped bars) of MDL 11,939 (10−6 M).
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Sci Rep
Mechanisms of 5-HT receptor antagonists in the regulation of fibrosis in a 3D human liver spheroid model. [Abstract]2024 Jan 16;14(1):1396. PMID: 38228622
Pimavanserin hemitartrate purchased from MedChemExpress. Usage Cited in: Sci Rep. 2024 Jan 16;14(1):1396. [Abstract]
Pimavanserin (1 μM) decreased COL1A1, TGF-β1, and vimentin deposition, although its effect was rather variable and thus non-significant.
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Int J Neuropsychopharmacol
A Complex Impact of Systemically Administered 5-HT2A Receptor Ligands on Conditioned Fear. [Abstract]2021 Sep 21;24(9):749-757. PMID: 34228806
Pimavanserin hemitartrate purchased from MedChemExpress. Usage Cited in: Int J Neuropsychopharmacol. 2021 Sep 21;24(9):749-757. [Abstract]
Number of animals per group = 11–12. a = P < .001 vs saline; b = P < .01 vs escitalopram; c = P < .01 vs pimavanserin (0.3 mg/kg).
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ACS Chem Neurosci
Big Data Challenges Targeting Proteins in GPCR Signaling Pathways; Combining PTML-ChEMBL Models and [35S]GTPγS Binding Assays. [Abstract]2019 Nov 20;10(11):4476-4491. PMID: 31618004 -
Food Chem Toxicol
Non-clinical pharmacology and toxicology studies of LPM6690061, a novel 5-hydroxytryptamine (5-HT)2A receptor inverse agonist. [Abstract]2023 Jun:176:113800. PMID: 37100235 -
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bioRxiv
Identification of 5-HT2A Receptor Signaling Pathways Responsible for Psychedelic Potential. [Abstract]2023 Jul 31:2023.07.29.551106. PMID: 37577474 -
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Solvent & Solubility
DMSO : 100 mg/mL (198.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (99.48 mM; Need ultrasonic)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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: ≥ 2.08 mg/mL (4.14 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.14 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocol
Rats: Thirty minutes before being placed in the startle apparatus, rats are treated with saline (s.c.), MDL-100,151 (1.0 mg/kg s.c.), or one of three doses of ACP-103 (1.0, 3.0, or 10.0 mg/kg s.c.). Five minutes after the pretreatment, rats are administered either DOI HCl (0.5 mg/kg s.c.) or 0.9% saline (s.c.). The acoustic startle session lasted approximately 37 min. After 1 week, rats are tested again in the same acoustic/tactile startle session in the exact order and at the same time as the previous week. The same pretreatment drug or vehicle is administered, and rats are crossed over to receive the treatment opposite to that they received the previous week (e.g., DOI HCl for week 1, 0.9% saline for week 2)[1].
Mice: Non-Swiss albino mice are used for locomotor activity experiments. For determination of spontaneous activity, ACP-103 is administered alone (s.c. 60 min before session start or p.o. 60 min before session start). For hyperactivity experiments, mice are treated with 0.3 mg/kg MK-801 (i.p.) 15 min presession (the peak dose for producing hyperactivity in an inverted-U dose-effect curve as determined in pilot experiments) in combination with vehicle or ACP-103. Motor activity data are collected during a 15-min session in a lit room[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 (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Vanover KE, et al. Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP- 103), a novel 5-hydroxytryptamine(2A) receptor inverse agonist. J Pharmacol Exp Ther. 2006 May;317(2):910-8. [Content Brief]
[2]. Ezzeldin E, et al. A rapid, simple and highly sensitive UPLC-MS/MS method for quantitation of pimavanserin in plasma and tissues: Application to pharmacokinetics and brain uptake studies in mice. J Chromatogr B Analyt Technol Biomed Life Sci. 2020 Apr 15;1143:122015. [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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.9897 mL | 9.9485 mL | 19.8969 mL | 49.7423 mL |
| 5 mM | 0.3979 mL | 1.9897 mL | 3.9794 mL | 9.9485 mL | |
| 10 mM | 0.1990 mL | 0.9948 mL | 1.9897 mL | 4.9742 mL | |
| 15 mM | 0.1326 mL | 0.6632 mL | 1.3265 mL | 3.3162 mL | |
| 20 mM | 0.0995 mL | 0.4974 mL | 0.9948 mL | 2.4871 mL | |
| 25 mM | 0.0796 mL | 0.3979 mL | 0.7959 mL | 1.9897 mL | |
| 30 mM | 0.0663 mL | 0.3316 mL | 0.6632 mL | 1.6581 mL | |
| 40 mM | 0.0497 mL | 0.2487 mL | 0.4974 mL | 1.2436 mL | |
| 50 mM | 0.0398 mL | 0.1990 mL | 0.3979 mL | 0.9948 mL | |
| 60 mM | 0.0332 mL | 0.1658 mL | 0.3316 mL | 0.8290 mL | |
| 80 mM | 0.0249 mL | 0.1244 mL | 0.2487 mL | 0.6218 mL | |
| DMSO | 100 mM | 0.0199 mL | 0.0995 mL | 0.1990 mL | 0.4974 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Pimavanserin hemitartrate Related Classifications
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