Fluoroclebopride
Based on 1 Customer Validation
Fluoroclebopride is a Dopamine receptor ligand with a binding Ki of 0.95 nM for the dopamine D2 receptor and a binding Ki of 5.46 nM for the dopamine D3 receptor. When radiolabeled with 18F, Fluoroclebopride can be used to detect the availability of dopamine D2 and D3 receptors in the caudate nucleus and putamen of primates.
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- Pureza : 99.90%
- No. CAS: 154540-49-5
- Fòrmula: C20H23ClFN3O2
- Peso molecular:391.87
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
D3 Receptor 5.46 nM (Ki) |
D2 Receptor 0.95 nM (Ki) |
In Vivo
Fluoroclebopride Chronic extensive tropane alkaloid stimulant self-administration produces a persistent >20% reduction in striatal dopamine D2 receptor availability, as measured by Fluoroclebopride PET, that does not reverse even after more than 7 months of enforced abstinence[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cynomolgus monkeys (adult male, experimentally naive, body weights maintained at approximately 95% of free-feeding weights)[1]
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Dosage:3-5 mCi
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Administration:bolus
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Result:Showed baseline [18F]fluoroclebopride DVRs in the caudate nucleus of 5 monkeys ranging from 2.22 to 3.07, and baseline putamen DVRs ranging from 2.78 to 3.29.
Exhibited post-treatment striatal (mean of caudate nucleus and putamen) DVR changes where monkeys with relatively low baseline DVRs showed increased DVR values, while monkeys with the highest baseline DVRs showed decreased DVR values across the 5 tested monkeys.
Demonstrated that 2 out of 9 total studied monkeys deviated from the general baseline-dependent DVR change pattern.
Chemical Information
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No. CAS 154540-49-5
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Appearance Solid
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Peso molecular 391.87
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Fòrmula C20H23ClFN3O2
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Color White to off-white
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SMILES
O=C(NC1CCN(CC2=CC=C(F)C=C2)CC1)C3=CC(Cl)=C(N)C=C3OC
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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 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : ≥ 125 mg/mL (318.98 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Working solution concentration: 0.22 mg/mL
Pureza y Documentación
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Ficha de datos (275 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Czoty PW, et al. Effects of repeated treatment with the dopamine D2/D3 receptor partial agonist aripiprazole on striatal D2/D3 receptor availability in monkeys. Psychopharmacology. 2013 Sep 29. [Content Brief]
[2]. Nader MA, et al. PET imaging of dopamine D2 receptors in monkey models of cocaine abuse: genetic predisposition versus environmental modulation. The American journal of psychiatry. 2005 Aug;162(8):1473-82. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5519 mL | 12.7593 mL | 25.5187 mL | 63.7967 mL |
| 5 mM | 0.5104 mL | 2.5519 mL | 5.1037 mL | 12.7593 mL | |
| 10 mM | 0.2552 mL | 1.2759 mL | 2.5519 mL | 6.3797 mL | |
| 15 mM | 0.1701 mL | 0.8506 mL | 1.7012 mL | 4.2531 mL | |
| 20 mM | 0.1276 mL | 0.6380 mL | 1.2759 mL | 3.1898 mL | |
| 25 mM | 0.1021 mL | 0.5104 mL | 1.0207 mL | 2.5519 mL | |
| 30 mM | 0.0851 mL | 0.4253 mL | 0.8506 mL | 2.1266 mL | |
| 40 mM | 0.0638 mL | 0.3190 mL | 0.6380 mL | 1.5949 mL | |
| 50 mM | 0.0510 mL | 0.2552 mL | 0.5104 mL | 1.2759 mL | |
| 60 mM | 0.0425 mL | 0.2127 mL | 0.4253 mL | 1.0633 mL | |
| 80 mM | 0.0319 mL | 0.1595 mL | 0.3190 mL | 0.7975 mL | |
| 100 mM | 0.0255 mL | 0.1276 mL | 0.2552 mL | 0.6380 mL |
Fluoroclebopride Related Classifications
HY-102089 Related Classifications
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Keywords
- Fluoroclebopride
- 154540-49-5
- Dopamine Receptor
- Radionuclide-Drug Conjugates (RDCs)
- cynomolgus monkeys
- benzoylmethylecgonine abuse
- dopamine D3 receptor
- benzoylmethylecgonine dependence
- dopamine D2 receptor
- tropane alkaloid stimulant
- nonhuman primates
- caudate nucleus
- positron emission tomography radiotracer
- putamen
- Inhibitor
- inhibitor
- inhibit