Raclopride
(Synonyms: 雷氯必利) 目录号 : GC16769
Raclopride是一种取代的苯甲酰胺，是具有高选择性的多巴胺D2 和D3受体拮抗剂。
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.
Raclopride是一种取代的苯甲酰胺，是具有高选择性的多巴胺D2 和D3受体拮抗剂 [1]。Raclopride对大脑多巴胺受体的选择性由其各自的Ki值表征决定，分别为：D2受体1.8nM，D3受体3.5nM，D4受体2400nM，D1受体18000nM。Raclopride主要用于神经系统疾病领域，包括精神分裂症[2]和帕金森病[3]。Raclopride能够穿过血脑屏障并结合大脑中的多巴胺受体，因此被广泛用于正电子发射断层扫描（PET）成像，以研究大脑中多巴胺受体的分布和密度[4]。
Raclopride（0.1、0.3或0.6mg/kg）处理显示出明显的剂量依赖性抗攻击效果，显著抑制了大鼠的隔离诱导攻击行为[5]。Raclopride（0.5mg/kg）处理可以预防C57BL6/J小鼠安非他明诱导的目标导向行为障碍[6]。
| 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 | |
| 别名 | 雷氯必利 | ||
| 化学名 | (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 | ||
| 分子式 | C15H20Cl2N2O3 | 分子量 | 347.24 |
| 溶解度 | DMF: 15 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 15 mg/ml,Ethanol: 1 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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