| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
5-HT2A (serotonin 2A) receptor. Altanserin is a highly specific 5-HT2A receptor antagonist. It binds to the 5-HT2A receptor with high affinity and selectivity, making it useful as a radioligand for PET imaging. The compound does not significantly bind to other serotonin receptor subtypes, ensuring specificity for 5-HT2A imaging.
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|---|---|
| ln Vitro |
Fluorine-18 artanserin can be used to manufacture artanserin[1].
Altanserin demonstrates high affinity and selectivity for the 5-HT2A receptor in vitro. It has been characterized in radioligand binding assays using membranes from cells expressing the 5-HT2A receptor. The compound's binding affinity (Ki) has been determined in various studies. It is used as a precursor for fluorine-18 radioligand synthesis. |
| ln Vivo |
In vivo, Altanserin is used as a PET radioligand to image 5-HT2A receptors in the brain. [18F]Altanserin binds to 5-HT2A receptors in living subjects, allowing non-invasive quantification of receptor density and occupancy. This has been used to study psychiatric disorders such as depression, schizophrenia, and anxiety, as well as neurological conditions.
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| Enzyme Assay |
In vitro receptor binding assays for Altanserin typically involve competition binding experiments using radiolabeled ligands such as [3H]-ketanserin or [3H]-MDL100907. Membranes are prepared from cells or tissues expressing the 5-HT2A receptor. Altanserin is incubated at varying concentrations, and bound radioactivity is measured. Ki values are calculated from displacement curves.
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| Cell Assay |
Cellular assays for Altanserin are not typically performed, as the compound is primarily used as a radioligand for imaging rather than a therapeutic agent. However, functional assays measuring 5-HT2A receptor-mediated signaling (e.g., calcium mobilization) may be used to confirm antagonist activity. Cells expressing the 5-HT2A receptor are treated with Altanserin, and receptor activation is measured.
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| Animal Protocol |
In vivo animal studies for Altanserin are typically PET imaging studies in rodents, non-human primates, or other species. The compound is radiolabeled with fluorine-18 and administered intravenously. Brain uptake and receptor binding are measured using PET scanners. Biodistribution studies may also be performed to assess off-target binding.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Altanserin are primarily derived from PET imaging studies. The compound is administered intravenously as a radioligand and distributes to the brain where it binds to 5-HT2A receptors. Its molecular weight is 411.49, and its molecular formula is C22H22FN3O2S. Detailed ADME parameters are not extensively documented.
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| Toxicity/Toxicokinetics |
Altanserin is a research compound and is not approved for human therapeutic use. As a radioligand, it is administered in trace amounts for imaging purposes and is generally considered safe at the doses used for PET imaging. Standard radiation safety precautions apply when using radiolabeled compounds. The compound is intended for research use only.
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| References | |
| Additional Infomation |
Altanserin belongs to the quinazoline class of compounds.
Altanserin is a selective 5-HT2A receptor antagonist used as a PET radioligand for brain imaging. [18F]Altanserin is used to study 5-HT2A receptors in psychiatric and neurological disorders. The compound is not approved for therapeutic use and is available only for research purposes. Its molecular formula is C22H22FN3O2S, and its molecular weight is 411.49. |
| Molecular Formula |
C22H22N3O2FS
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|---|---|
| Molecular Weight |
411.49238
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| Exact Mass |
411.142
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| CAS # |
76330-71-7
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| Related CAS # |
Altanserin hydrochloride;1135280-78-2
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| PubChem CID |
3033677
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| Appearance |
White to light yellow solid powder
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| Density |
1.37 g/cm3
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| Boiling Point |
601ºC at 760 mmHg
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| Flash Point |
317.3ºC
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| Index of Refraction |
1.674
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| LogP |
3.731
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
630
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SMYALUSCZJXWHG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H22FN3O2S/c23-17-7-5-15(6-8-17)20(27)16-9-11-25(12-10-16)13-14-26-21(28)18-3-1-2-4-19(18)24-22(26)29/h1-8,16H,9-14H2,(H,24,29)
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| Chemical Name |
3-[2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl]-2-sulfanylidene-1H-quinazolin-4-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~19.23 mg/mL (~46.73 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.92 mg/mL (4.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 19.2 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4302 mL | 12.1510 mL | 24.3019 mL | |
| 5 mM | 0.4860 mL | 2.4302 mL | 4.8604 mL | |
| 10 mM | 0.2430 mL | 1.2151 mL | 2.4302 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01398189 | Unknown status | Drug: clozapine | Schizoaffective Disorder Schizophrenia |
Seoul National University Bundang Hospital | 2011-07 | Not Applicable |
| NCT03970239 | Unknown status | Drug: Positron Emission Tomography using [11 Carbon]-3-amino-4-(2-dimethylaminomethylphenylsulfanyl)- benzonitrile ([11C]-DASB) and [18 Fluorine]-altanserin ([18F]-altanserin) Drug: Positron Emission Tomography using [18 Fluorine]-altanserin ([18F]-altanserin) |
Impulse Control Disorders Parkinson Disease |
Hospices Civils de Lyon | 2019-05-13 | Not Applicable |
| NCT01296802 | Completed | Drug: dexfenfluramine | Amphetamine Abuse Amphetamine-Related Disorders |
University of Zurich | 2006-04 | Not Applicable |
| NCT05942716 | Not yet recruiting | Drug: Administration of a PET radiotracer |
Tourette Disorder | Hospices Civils de Lyon | 2023-12-01 | Phase 2 |
| NCT00581282 | Withdrawn | Radiation: PET scan Other: fMRI |
Substance Abuse Disorder | University of California, Irvine | 2005-12 |
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