Abaperidone
(Synonyms: 阿巴哌酮) 目录号 : GC31055
Abaperidone是一种有效的5-HT2A受体和多巴胺D2受体拮抗剂，IC50分别为6.2和17nM。
Cas No.:183849-43-6
Sample solution is provided at 25 µL, 10mM.
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Abaperidone is a potent antagonist of 5-HT2A receptor and dopamine D2 receptor with IC50s of 6.2 and 17 nM.
Abaperidone possesses good affinity for dopamine D2 receptors, together with a greater affinity for 5-HT2 receptors with IC50 of 17 and 6.2 nM, reaspectively[1].
The time course of the inhibition of climbing behavior for a period of several hours after oral administration of either 0.5 mg/kg of Abaperidone or risperidone is tested in mice. Also is included a comparative test of catalepsy induced by Abaperidone and risperidone along several hours following oral administration at several doses in rats. A somewhat lesser induction of catalepsy is observed for Abaperidone. A study of serum prolactin levels after oral administration of Abaperidone, haloperidol, and risperidone at 5 mg/kg for either 1 or 3 days in rats. Increases in prolactin levels after oral administration of Abaperidone are smaller than those for reference drugs[1].
[1]. Bolós J, et al. 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). J Med Chem. 1998 Dec 31;41(27):5402-9.
Kinase experiment: | Receptor binding assays are performed by inhibition of radioligand binding according to reported procedures for D1, D2, D3, D4, 15a5-HT1A, 5-HT2A, α1, α2, β, muscarinic, and σ receptors. IC50 values are calculated from concentration−response curves at 11 different concentrations of the test compound, each done in duplicate[1]. |
Animal experiment: | Rats[1] Sprague-Dawley rats (220-240 g) are assigned to 8 groups of 5 animals each, and are orally dosed with either Abaperidone (5 mg/kg/day), Haloperidol (5 mg/kg/day), Risperidone (5 mg/kg/day), or the vehicle for 1 or 3 consecutive days. The animals are killed by decapitation 3 h after last dosing, blood samples of 2 mL are collected, and prolactin levels are determined by means of an EIA kit from Amersham. |
References: [1]. Bolós J, et al. 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). J Med Chem. 1998 Dec 31;41(27):5402-9. | |
| Cas No. | 183849-43-6 | SDF | |
| 别名 | 阿巴哌酮 | ||
| Canonical SMILES | O=C1C(CO)=COC2=CC(OCCCN3CCC(C4=NOC5=C4C=CC(F)=C5)CC3)=CC=C12 | ||
| 分子式 | C25H25FN2O5 | 分子量 | 452.47 |
| 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 | 2.2101 mL | 11.0505 mL | 22.1009 mL |
| 5 mM | 0.442 mL | 2.2101 mL | 4.4202 mL |
| 10 mM | 0.221 mL | 1.105 mL | 2.2101 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet