1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. 5-HT2A inverse agonist-1

5-HT2A inverse agonist-1 是一种5-HT2A 受体反向激动剂,其 IC50 值为 5.5 nM。5-HT2A inverse agonist-1 对 hERG 的抑制作用极小。5-HT2A inverse agonist-1 可用于神经系统疾病的研究,如帕金森病。

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5-HT2A inverse agonist-1

5-HT2A inverse agonist-1 Chemical Structure

CAS No. : 3028943-38-3

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  • 生物活性

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生物活性

5-HT2A inverse agonist-1 is a 5-HT2A receptor inverse agonist with a IC50 of 5.5 nM. 5-HT2A inverse agonist-1 shows minimal hERG inhibition. 5-HT2A inverse agonist-1 can be used for the research of neurological disease, such as Parkinson’s disease[1].

IC50 & Target[1]

5-HT2A Receptor

5.5 nM (IC50)

体内研究
(In Vivo)

5-HT2A inverse agonist-1 (Compound P25a) (0.47-4.27 μmol/kg,灌胃) 可减轻 DOI 诱导的头部抽搐大鼠模型的头部抽搐症状[1]
5-HT2A inverse agonist-1 (0.51-5.1 μmol/kg,灌胃) 能减少 MK801 (HY-15084B) 诱导的活动亢进大鼠模型的活动距离[1]

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

Animal Model: DOI-induced head twitches rats models[1]
Dosage: 0.47, 1.41, 4.27 μmol/kg
Administration: Orally gavage
Result: Reduced numbers of head twitches.
Animal Model: MK801-induced hyperactivity rats models[1]
Dosage: 0.51, 1.7 and 5.1 μmol/kg
Administration: Orally gavage
Result: Decreases activity distance.
分子量

472.45

Formula

C22H25F5N4O2

CAS 号
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.

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参考文献
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    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:
5-HT2A inverse agonist-1
目录号:
HY-175822
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