Lusaperidone (R107474)
(Synonyms: R107474) 目录号 : GC31266
Lusaperidone (R107474) (R107474) 是一种 α2 肾上腺素能受体拮抗剂，α2A 和 α2C 的 Kis 分别为 0.13 和 0.15 nM。
Cas No.:214548-46-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Rats: Radio labeled Lusaperidone (24–28 GBq/μmol) is injected into the tail vein of diethyl ether anesthetized male Wistar rats (200–250 g). The rats received 30–40 MBq (injected at the start of the experiment) in 300 μL saline including 10% (v/v) ethanol. The rats are sacrificed by cervical dislocation at 5, 10, 20, and 30 min post injection under diethyl ether anesthesia. A blood sample is taken by cardiac puncture and selected tissues are rapidly dissected and weighed. The radioactivity is measured[1]. |
References: [1]. Van der Mey M, et al. Synthesis and biodistribution of [11C]R107474, a new radiolabeled alpha2-adrenoceptor antagonist. Bioorg Med Chem. 2006 Jul 1;14(13):4526-34. | |
Lusaperidone (R107474) is an α2 adrenergic receptor antagonist with Kis of 0.13 and 0.15 nM for α2A and α2C, respectively.
Lusaperidone has subnanomolar affinity for α2A and α2C adrenergic receptor (Ki=0.13 and 0.15 nM, respectively) and shows nanomolar affinity for the hα2B adrenergic receptor and h5-HT7 receptors (Ki=1 and 5 nM, respectively). Lusaperidone interacts weakly (Ki values ranging between 81 and 920 nM) with dopamine-hD2L, -hD3 and -hD4, h5-HT1D-, h5-HT1F-, h5-HT2A-, h5-HT2C-, and h5-HT5A receptors. Lusaperidone, tested up to 10 μM, interacts only at micromolar concentrations or not at all with any of the other receptor or transporter binding sites tested in this study. Lusaperidone has been shown to reverse the clonidine-induced inhibition of cyclic AMP production mediated by human α2A and α2C adrenoceptors expressed in cell lines (Kb is 2.8 and 4.4 nM, respectively) and is a full antagonist on both receptor subtypes[1].
Lusaperidone occupies the α2A and α2C adrenergic receptor with an ED50 of 0.014 mg/kg sc (0.009-0.019) and 0.026 mg/kg sc (0.022-0.030), respectively. The uptake of R107474 after in vivo intravenous administration is very rapid; in most tissues (including the brain) it reaches maximum concentration at 5 min after tracer injection[1].
[1]. Van der Mey M, et al. Synthesis and biodistribution of [11C]R107474, a new radiolabeled alpha2-adrenoceptor antagonist. Bioorg Med Chem. 2006 Jul 1;14(13):4526-34.
| Cas No. | 214548-46-6 | SDF | |
| 别名 | R107474 | ||
| Canonical SMILES | O=C1C(CCN2CCC(OC3=CC=CC=C34)=C4C2)=C(C)N=C5N1C=CC=C5 | ||
| 分子式 | C22H21N3O2 | 分子量 | 359.42 |
| 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 | 2.7823 mL | 13.9113 mL | 27.8226 mL |
| 5 mM | 0.5565 mL | 2.7823 mL | 5.5645 mL |
| 10 mM | 0.2782 mL | 1.3911 mL | 2.7823 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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