Raclopride (Synonyms: (S)-(-)-Raclopride) |
| Catalog No.GC16769 |
Raclopride is a substituted benzamide with high selectivity as an antagonist of dopamine D2 and D3 receptors.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 84225-95-6
Sample solution is provided at 25 µL, 10mM.
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Raclopride is a substituted benzamide with high selectivity as an antagonist of dopamine D2 and D3 receptors[1]. The selectivity of Raclopride for dopamine receptors is determined by its respective Ki values, which are as follows: 1.8, 3.5, 2400, and 18000 nM for D2, D3, D4, and D1 receptors respectively. Raclopride is mainly used in the field of neurological disorders, including schizophrenia[2] and Parkinson's disease[3]. Raclopride can cross the blood-brain barrier and bind to dopamine receptors in the brain, so it is widely used in positron emission tomography (PET) imaging to study the distribution and density of dopamine receptors in the brain[4][5].
Raclopride (0.1, 0.3, or 0.6mg/kg) treatment exhibits a clear dose-dependent anti-aggressive effect, significantly inhibiting isolation-induced aggression in rats[6]. Raclopride (0.5mg/kg) can prevent the amphetamine-induced impairment in goal-directed action of C57BL6/J mice[7].
References:
[1]. Farde L, Pauli S, Hall H, et al. Stereoselective binding of 11C-raclopride in living human brain--a search for extrastriatal central D2-dopamine receptors by PET. Psychopharmacology (Berl). 1988;94(4):471-8. doi: 10.1007/BF00212840. PMID: 3131792.
[2]. Farde L, Wiesel FA, Stone-Elander S, et al. D2 dopamine receptors in neuroleptic-naive schizophrenic patients. A positron emission tomography study with [11C]raclopride. Arch Gen Psychiatry. 1990 Mar;47(3):213-9. doi: 10.1001/archpsyc.1990.01810150013003. PMID: 1968328.
[3]. Antonini A, Schwarz J, Oertel WH, et al. Long-term changes of striatal dopamine D2 receptors in patients with Parkinson's disease: a study with positron emission tomography and [11C]raclopride. Mov Disord. 1997 Jan;12(1):33-8. doi: 10.1002/mds.870120107. PMID: 8990051.
[4]. Schlaepfer TE, Pearlson GD, Wong DF, et al. PET study of competition between intravenous cocaine and [11C]raclopride at dopamine receptors in human subjects. Am J Psychiatry. 1997 Sep;154(9):1209-13. doi: 10.1176/ajp.154.9.1209. PMID: 9286178.
[5]. Roux GL, Jarray R, Guyot AC, et al. Proof-of-Concept Study of Drug Brain Permeability Between in Vivo Human Brain and an in Vitro iPSCs-Human Blood-Brain Barrier Model. Sci Rep. 2019 Nov 5;9(1):16310. doi: 10.1038/s41598-019-52213-6. PMID: 31690750; PMCID: PMC6831611.
[6]. Aguilar MA, Miñarro J, Pérez-Iranzo N, et al. Behavioral profile of raclopride in agonistic encounters between male mice. Pharmacol Biochem Behav. 1994 Mar;47(3):753-6. doi: 10.1016/0091-3057(94)90185-6. PMID: 7911581.
[7]. Conn KA, Alexander S, Burne THJ, et al. Antagonism of D2 receptors via raclopride ameliorates amphetamine-induced associative learning deficits in male mice. Behav Brain Res. 2023 Oct 2;454:114649. doi: 10.1016/j.bbr.2023.114649. Epub 2023 Aug 27. PMID: 37643667.
| Animal experiment [1]: | |
Animal models | C57BL6/J mice |
Preparation Method | Mice were administered Raclopride (0.5mg/kg) 30min prior to amphetamine injection that was completed 20 min prior to testing. Then the learning of action-outcomes was assessed by behavioural and operant testing. |
Dosage form | 0.5mg/kg, 14d, i.p. |
Applications | Raclopride treatment can block the amphetamine-induced impairment goal-directed action of mice. |
References: | |
| Cas No. | 84225-95-6 | SDF | |
| Synonyms | (S)-(-)-Raclopride | ||
| Chemical Name | (S)-3,5-dichloro-N-((1-ethylpyrrolidin-2-yl)methyl)-2-hydroxy-6-methoxybenzamide | ||
| Canonical SMILES | ClC1=C(C(C(NC[C@H]2N(CC)CCC2)=O)=C(C(Cl)=C1)O)OC | ||
| Formula | C15H20Cl2N2O3 | M.Wt | 347.24 |
| Solubility | DMF: 15 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 15 mg/ml,Ethanol: 1 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8799 mL | 14.3993 mL | 28.7985 mL |
| 5 mM | 0.576 mL | 2.8799 mL | 5.7597 mL |
| 10 mM | 0.288 mL | 1.4399 mL | 2.8799 mL |
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Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.50%
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Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)
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