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Raclopride (formerly FLA 870) is a novel, potent and selective dopamine D2/D3 receptor antagonist, which binds to D2 and D3 receptors with dissociation constants (Kis) of 1.8 nM and 3.5 nM, respectively, but has a very low affinity for D1 and D4 receptors with Kis of 18000 nM and 2400 nM, respectively. Raclopride's selectiveness for cerebral D2 receptors is indicated by its Ki-values, which are 1.8, 3.5, 2400, and 18000 nM for D2, D3, D4, and D1 receptors, respectively. It can be radiolabelled with radioisotopes, such as 3H or 11C, and used as a tracer for positron emission tomography (PET) and in vitro imaging (autoradiography). The non-invasive evaluation of the binding capacity of the cerebral D2 dopamine receptor is made possible by images acquired by cerebral PET scanning (e.g., PET/CT or PET/MRI), which can be helpful in the diagnosis of movement disorders.
| Targets |
D2 Receptor ( Ki = 1.8 nM ); D3 Receptor ( Ki = 3.5 nM ); D4 Receptor ( Ki = 2400 nM ); D1 Receptor ( Ki = 18000 nM )
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|---|---|
| ln Vivo |
Raclopride (0.1, 0.3, or 0.6 mg/kg; IP; 30 min; albino male mice; OF1 strain) dramatically shortens the amount of time that the mice spend engaging in aggressive behavior[2].
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| Animal Protocol |
Albino male mice of the OF1 strain
0.1, 0.3, or 0.6 mg/kg i.p. |
| References |
| Molecular Formula |
C₁₅H₂₀CL₂N₂O₃
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|---|---|
| Molecular Weight |
347.24
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| Exact Mass |
346.09
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| CAS # |
84225-95-6
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| Related CAS # |
Raclopride-d5 hydrochloride; 1217623-85-2; Raclopride tartrate; 98185-20-7
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| Appearance |
Powder
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| SMILES |
CCN1CCC[C@H]1CNC(=O)C2=C(C(=CC(=C2OC)Cl)Cl)O
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| InChi Key |
WAOQONBSWFLFPE-VIFPVBQESA-N
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| InChi Code |
InChI=1S/C15H20Cl2N2O3/c1-3-19-6-4-5-9(19)8-18-15(21)12-13(20)10(16)7-11(17)14(12)22-2/h7,9,20H,3-6,8H2,1-2H3,(H,18,21)/t9-/m0/s1
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| Chemical Name |
3,5-dichloro-N-[[(2S)-1-ethylpyrrolidin-2-yl]methyl]-2-hydroxy-6-methoxybenzamide
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| Synonyms |
FLA 870; FLA-870; FLA870; Raclopride
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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: 69~100 mg/mL (198.7~288 mM)
Ethanol: ~69 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.20 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.20 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.20 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8799 mL | 14.3993 mL | 28.7985 mL | |
| 5 mM | 0.5760 mL | 2.8799 mL | 5.7597 mL | |
| 10 mM | 0.2880 mL | 1.4399 mL | 2.8799 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 |
| NCT05282277 | Recruiting | Drug: Transdermal Estradiol Drug: Raclopride C11 |
Depression Psychosis Anhedonia |
University of North Carolina, Chapel Hill |
April 20, 2022 | Phase 4 |
| NCT02169310 | Recruiting | Device: tDCS Drug: [11C] Raclopride |
Traumatic Brain Injury | National Institute of Neurological Disorders and Stroke (NINDS) |
November 18, 2014 | Phase 1 |
| NCT03190954 | Recruiting | Drug: [11C]raclopride plus placebo Drug: [11C]raclopride plus drug |
Normal Physiology Opioid Use Disorders |
National Institute on Alcohol Abuse and Alcoholism (NIAAA) |
August 17, 2017 | Early Phase 1 |
| NCT03648892 | Completed | Drug: [c11] raclopride Drug: [18F]fallypride |
Obesity Overweight Healthy Volunteers |
National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) |
September 21, 2018 | Early Phase 1 |
| NCT02020408 | Completed | Drug: [11C]raclopride Drug: [11C]DASB Drug: amphetamine |
Eating Disorder | University of California, San Diego |
May 2011 | Phase 4 |
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