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| Targets |
Fallypride targets dopamine D2 and D3 receptors, which are G protein-coupled receptors that play critical roles in the regulation of movement, motivation, reward, and cognition. Dopamine D2/D3 receptors are implicated in various neurological and psychiatric disorders, including schizophrenia, Parkinson's disease, and addiction. As a potent antagonist, Fallypride binds to these receptors and blocks dopamine-mediated signaling. When labeled with fluorine-18, Fallypride serves as a PET radiotracer for non-invasive imaging of D2/D3 receptor availability in the living human brain.
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| ln Vitro |
As a PET radiotracer, Fallypride (18F) shows high affinity and selectivity for dopamine D2/D3 receptors, enabling sensitive and specific imaging of these receptors in the brain. The unlabeled compound Fallypride is a potent antagonist of dopamine D2/D3 receptors. The compound's binding properties have been extensively characterized in vitro using radioligand binding assays.
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| ln Vivo |
In vivo activity of Fallypride (18F) has been demonstrated in PET imaging studies in humans and animal models. The radiotracer enables quantification of dopamine D2/D3 receptor availability and occupancy in the brain. Fallypride (18F) is under investigation in clinical trial NCT02310360 for studying striatal and extra-striatal dopamine release in response to food in healthy humans.
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| Enzyme Assay |
Non-cell-based binding assays for Fallypride typically involve measuring the affinity of the compound for dopamine D2 and D3 receptors using radioligand binding assays. A standard protocol includes: preparing membrane preparations from cells expressing dopamine D2 or D3 receptors, incubating with a radiolabeled ligand (such as [3H]spiperone or [3H]raclopride), adding Fallypride at various concentrations, and measuring displacement of the radioligand to determine binding affinity (Ki). IC50 values are calculated from competition binding curves.
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| Cell Assay |
Cellular assays for Fallypride are not typically performed as the compound is primarily used as a PET radiotracer. However, functional assays measuring dopamine receptor-mediated signaling (such as cAMP accumulation or β-arrestin recruitment) could be used to confirm antagonist activity. A representative protocol includes: culturing cells expressing dopamine D2 or D3 receptors, treating with Fallypride at various concentrations, and measuring inhibition of dopamine-induced signaling.
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| Animal Protocol |
In vivo animal studies with Fallypride (18F) typically involve PET imaging in rodent or non-human primate models. A typical protocol includes: intravenous administration of Fallypride (18F), dynamic PET scanning to measure radiotracer distribution in the brain, and quantification of binding potential (BPND) using kinetic modeling. The radiotracer is used to measure dopamine D2/D3 receptor availability and occupancy under various conditions.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Fallypride have been characterized for PET imaging applications. The compound has a molecular weight of 364.45 g/mol. Fallypride is a colorless to light yellow liquid with a density of 1.079 g/cm3. Storage: Powder at -20°C for 3 years, 4°C for 2 years; in solvent at -80°C for 6 months, -20°C for 1 month. Solubility: Typically soluble in DMSO (e.g., 10 mM).
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| Toxicity/Toxicokinetics |
As a PET radiotracer, Fallypride (18F) is used in clinical and preclinical research settings. The compound has been evaluated for safety in human studies, including clinical trial NCT02310360. Appropriate radiation safety precautions should be followed when handling the radiolabeled form of the compound. The unlabeled compound is for research use only.
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| References | |
| Additional Infomation |
Fallypride is being studied in the clinical trial NCT02310360 (Striatum and extrastriatum dopamine release response in healthy humans to food).
Fallypride (CAS 166173-78-0) is a potent antagonist of dopamine D2/D3 receptors. Fallypride (18F) is a positron emission tomography (PET) radiotracer used for imaging dopamine D2/D3 receptors in the brain. The compound is under investigation in clinical trial NCT02310360 for studying striatal and extra-striatal dopamine release in response to food in healthy humans. Fallypride is available as a research reagent for neuroscience and PET imaging applications. |
| Molecular Formula |
C20H29FN2O3
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|---|---|
| Molecular Weight |
364.45
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| Exact Mass |
364.216
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| Elemental Analysis |
C, 65.91; H, 8.02; F, 5.21; N, 7.69; O, 13.17
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| CAS # |
166173-78-0
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| PubChem CID |
10021692
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| Appearance |
Colorless to light yellow liquid（Density：1.079±0.06 g/cm3）
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| Density |
1.079 g/cm3
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| Boiling Point |
451.8ºC at 760 mmHg
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| Flash Point |
227ºC
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| LogP |
3.314
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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 |
10
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| Heavy Atom Count |
26
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| Complexity |
449
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| Defined Atom Stereocenter Count |
1
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| SMILES |
COC1=CC(=CC(=C1OC)C(=O)NC[C@@H]2CCCN2CC=C)CCCF
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| InChi Key |
OABRYNHZQBZDMG-INIZCTEOSA-N
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| InChi Code |
InChI=1S/C20H29FN2O3/c1-4-10-23-11-6-8-16(23)14-22-20(24)17-12-15(7-5-9-21)13-18(25-2)19(17)26-3/h4,12-13,16H,1,5-11,14H2,2-3H3,(H,22,24)/t16-/m0/s1
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| Chemical Name |
5-(3-fluoropropyl)-2,3-dimethoxy-N-[[(2S)-1-prop-2-enylpyrrolidin-2-yl]methyl]benzamide
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| Synonyms |
Fallypride; 166173-78-0; G9FWZ369GX; DTXSID30937173; Benzamide, 5-(3-fluoropropyl)-2,3-dimethoxy-N-(((2S)-1-(2-propen-1-yl)-2-pyrrolidinyl)methyl)-;
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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) |
Typically soluble in DMSO (e.g. 10 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7439 mL | 13.7193 mL | 27.4386 mL | |
| 5 mM | 0.5488 mL | 2.7439 mL | 5.4877 mL | |
| 10 mM | 0.2744 mL | 1.3719 mL | 2.7439 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.
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