1. GPCR/G Protein Neuronal Signaling
  2. Dopamine Receptor 5-HT Receptor
  3. Abaperidone

Abaperidone  (Synonyms: 阿巴哌酮)

目录号: HY-101619
产品使用指南

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 17 nM。

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Abaperidone Chemical Structure

Abaperidone Chemical Structure

CAS No. : 183849-43-6

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1 mg ¥3995
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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Abaperidone is a potent antagonist of 5-HT2A receptor and dopamine D2 receptor with IC50s of 6.2 and 17 nM.

IC50 & Target

D2 Receptor

17 nM (IC50)

5-HT2A Receptor

6.2 nM (IC50)

体外研究
(In Vitro)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

452.47

Formula

C25H25FN2O5

CAS 号
中文名称

阿巴哌酮

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
Kinase Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
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This equation is commonly abbreviated as: C1V1 = C2V2

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Abaperidone
目录号:
HY-101619
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