NRA-0160
目录号 : GC31015
NRA-0160是一种选择性的dopamineD4receptor拮抗剂，Ki值为0.48nM；同时对dopamineD2receptor，D3receptor，大鼠5-HT2Areceptor和α1adrenoceptor分别具有不同程度的亲和度，Ki值分别为>10000nM，39nM，180nM和237nM。
Cas No.:204718-47-8
Sample solution is provided at 25 µL, 10mM.
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NRA-0160 is a selective dopamine D4 receptor antagonist, with a Ki value of 0.48 nM and with negligible affinity for dopamine D2 receptor (Ki: >10000 nM), D3 receptor (Ki: 39 nM), rat 5-HT2A receptor (Ki: 180 nM) and rat α1 adrenoceptor (Ki: 237 nM).
NRA0160 (0.1, 1, or 3 mg/kg, i.p.) has no effect on PCP-induced hyperlocomotion, stereotypy or ataxia in SD rats. NRA0160, at any dose, does not reduce cumulated counts of locomotion and cumulated scores of stereotypy emerging, and has no effect on extracellular glutamate levels and locomotor activity emerged after saline injection[1]. NRA0160 dose-dependently and significantly reverses the effects of MAP on both A9 and Al0 dopamine neurons. NRA0160 is slightly more potent in reversiig the effects of MAP on A10 (ED50 = 1.0 mg/kg) than on A9 dopamine neurons (ED50 = 1.3 mg/kg). NRA0160 reverses the effect of AP0 on both A9 and A10 dopamine neurons. ED50 values for the effects of NRA0160 on APO-induced inhibition of A9 and A10 dopamine neurons are 1.3 mg/kg and 0.5 mg/kg, respectively[2].
[1]. Abekawa T, et al. Effects of NRA0045, a novel potent antagonist at dopamine D4, 5-HT2A, and alpha1 adrenaline receptors, and NRA0160, a selective D4 receptor antagonist, on phencyclidine-induced behavior and glutamate release in rats. Psychopharmacology (Berl). 2003 Sep;169(3-4):247-56. Epub 2003 Jul 31. [2]. Kawashima N, et al. Effects of selective dopamine D4 receptor blockers, NRA0160 and L-745,870, on A9 and A10 dopamine neurons in rats. Life Sci. 1999;65(24):2561-71.
Animal experiment: | Methamphetamine (MAP, 1 mg/kg, iv) or apomorphine (APO, 40 μg/kg iv.) and incremental doses of NRA0160 or G745870 (the starting dose is 0.1 mg/kg with sequential doses of 0.2, 0.7 and 2 mg/kg) are administered every 2-3 min (drug-induced changes usually reached their plateaus in 2-3 min) via an i.v. catheter implanted in the femoral vein of rats. Drug-induced changes (after reaching plateau) in neuronal activities which are plotted as percent changes from the preinjection baseline rate, are recorded over a 5 min period and defined as 100%. The % inhibition is calculated and ED50 values are determined. The ED50 values are analyzed by fitting it to the four parametric logistic functions, using non-linear least square regression (-) Apomorphine hydrochloride, methamphetamine HCl and L 745870 3HCl are dissolved in 0.9% saline with the addition of 0.1% ascorbic acid for apomorphine. NRA0160 is dissolved in a minimal amount of 0.5N HCl and distilled water for injection, then titrated is with 0.5N NaOH to a final pH of 5. |
References: [1]. Abekawa T, et al. Effects of NRA0045, a novel potent antagonist at dopamine D4, 5-HT2A, and alpha1 adrenaline receptors, and NRA0160, a selective D4 receptor antagonist, on phencyclidine-induced behavior and glutamate release in rats. Psychopharmacology (Berl). 2003 Sep;169(3-4):247-56. Epub 2003 Jul 31. | |
| Cas No. | 204718-47-8 | SDF | |
| Canonical SMILES | O=C(C1=NC(C2=CC=C(F)C=C2)=C(CCN3CC/C(CC3)=C\C4=CC=CC(F)=C4)S1)N | ||
| 分子式 | C24H23F2N3OS | 分子量 | 439.52 |
| 溶解度 | Soluble in DMSO | 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 | 2.2752 mL | 11.376 mL | 22.7521 mL |
| 5 mM | 0.455 mL | 2.2752 mL | 4.5504 mL |
| 10 mM | 0.2275 mL | 1.1376 mL | 2.2752 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
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: >98.00%
- COA (Certificate Of Analysis)
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