| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Raclopride (formerly also known as 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 corresponding Ki-values for D2, D3, D4, and D1 receptors are 1.8, 3.5, 2400, and 18000 nM, respectively, indicating its selectivity to the cerebral D2 receptors. It can be radiolabelled using 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 cerebral D2 dopamine receptor's binding capacity is made possible by images acquired through 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 )
|
|---|---|
| ln Vivo |
Raclopride tartrate (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].
Raclopride is a substituted benzamide with high selectivity as an antagonist of central dopaminergic D2 receptors and potential antipsychotic effects. In comparison with a classic DA receptor blocking agent like haloperidol, raclopride displays an atypical profile in preclinical tests for extrapyramidal side effects. Antiaggressive properties of raclopride on agonistic behavior have not yet been fully explored. In this work the effects of raclopride (0.1, 0.3, or 0.6 mg/kg) on aggressive and motor behaviors in male mice were studied. Aggression tests were performed 30 min after injections. Encounters were videotaped and behavior was evaluated, measuring the time spent in 11 broad categories of behavior. The results show a clear antiaggressive effect of raclopride, with very little motor impairment and some increase in exploratory behavior. This behavioral profile is very similar to the one observed with other atypical neuroleptics and differs somewhat from that found in the classic compounds.[2] |
| References | |
| Additional Infomation |
3,5-dichloro-N-[[(2S)-1-ethyl-2-pyrrolidinyl]methyl]-2-hydroxy-6-methoxybenzamide is a member of salicylamides.
Raclopride has been used in trials studying Parkinson Disease. A substituted benzamide that has antipsychotic properties. It is a dopamine D2 receptor (see RECEPTORS, DOPAMINE D2) antagonist. Dopamine receptors are the primary targets in the treatment of schizophrenia, Parkinson's disease, and Huntington's chorea, and are discussed in this review by Philip Seeman and Hubert Van Tol. Improved therapy may be obtained by drugs that selectively target a particular subtype of dopamine receptor. Most antipsychotic drugs block D2 receptors in direct correlation to clinical potency, except clozapine, which prefers D4 receptors. D1 and D2 receptors can enhance each other's actions, possibly through subunits of the G proteins. In schizophrenia, the D2 and D3 receptor density is elevated by 10%, while the D4 receptor density is elevated by 600%. Therefore, D4 receptors may be a target for future antipsychotic drugs. While antipsychotics originally helped to discover dopamine receptors, the five cloned dopamine receptors are now facilitating the discovery of selective antipsychotic and antiparkinson drugs. Antipsychotic Agents Agents that control agitated psychotic behavior, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect. They are used in SCHIZOPHRENIA; senile dementia; transient psychosis following surgery; or MYOCARDIAL INFARCTION; etc. These drugs are often referred to as neuroleptics alluding to the tendency to produce neurological side effects, but not all antipsychotics are likely to produce such effects. Many of these drugs may also be effective against nausea, emesis, and pruritus. (See all compounds classified as Antipsychotic Agents.) Dopamine Antagonists Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME. |
| Molecular Formula |
C19H26CL2N2O9
|
|---|---|
| Molecular Weight |
497.32374
|
| Exact Mass |
496.102
|
| Elemental Analysis |
C, 45.89; H, 5.27; Cl, 14.26; N, 5.63; O, 28.95
|
| CAS # |
98185-20-7
|
| Related CAS # |
Raclopride; 84225-95-6
|
| PubChem CID |
16219926
|
| Appearance |
Solid powder
|
| LogP |
1.127
|
| Hydrogen Bond Donor Count |
6
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
32
|
| Complexity |
520
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
CC[NH+]1CCC[C@H]1CNC(=O)c2c(c(cc(c2OC)Cl)Cl)O.[C@@H]([C@H](C(=O)[O-])O)(C(=O)O)O
|
| InChi Key |
QULBVRZTKPQGCR-NDAAPVSOSA-N
|
| InChi Code |
InChI=1S/C15H20Cl2N2O3.C4H6O6/c1-3-19-6-4-5-9(19)8-18-15(21)12-13(20)10(16)7-11(17)14(12)22-2;5-1(3(7)8)2(6)4(9)10/h7,9,20H,3-6,8H2,1-2H3,(H,18,21);1-2,5-6H,(H,7,8)(H,9,10)/t9-;1-,2-/m01/s1
|
| Chemical Name |
3,5-dichloro-N-[[(2S)-1-ethylpyrrolidin-2-yl]methyl]-2-hydroxy-6-methoxybenzamide;(2R,3R)-2,3-dihydroxybutanedioic acid
|
| Synonyms |
Raclopride; FLA-870; FLA870; Raclopride tartrate; 98185-20-7; EXZ5FGZ55J; Raclopride (tartrate); UNII-EXZ5FGZ55J; 98185-20-7 (tartrate); (S)-3,5-dichloro-N-((1-ethylpyrrolidin-2-yl)methyl)-2-hydroxy-6-methoxybenzamide (2R,3R)-2,3-dihydroxysuccinate; (S)-(-)-3,5-Dichloro-N-((1-ethyl-2-pyrrolidinyl)methyl)-6-methoxysalicylamide L-(+)-tartrate; FLA 870; Raclopride tartrate
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~288 mM)
H2O: ~0.1 mg/mL (~0.3 mM) |
|---|---|
| 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 | 2.0108 mL | 10.0539 mL | 20.1078 mL | |
| 5 mM | 0.4022 mL | 2.0108 mL | 4.0216 mL | |
| 10 mM | 0.2011 mL | 1.0054 mL | 2.0108 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 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA