1. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel
  2. 5-HT Receptor Adrenergic Receptor GABA Receptor Serotonin Transporter Dopamine Receptor
  3. CSP-2503

CSP-2503 是一种强效且选择性的 5-HT1A 受体激动剂,其 EC50 为 0.15 μM,Ki 为 4.1 nM。CSP-2503 在 α1-肾上腺素能受体 (α1-adrenoceptors) (Ki > 1000 nM)、5-HT4 受体和苯二氮䓬受体上表现出优异的选择性。CSP-2503 在体外抑制 cAMP 的增加,并在体内表现出抗焦虑活性。CSP-2503 可用于焦虑相关障碍的研究。

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CSP-2503

CSP-2503 Chemical Structure

CAS No. : 581813-10-7

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CSP-2503 is a potent and selective 5-HT1A receptor agonist , with an EC50 of 0.15 μM and a Ki of 4.1 nM. CSP-2503 exhibits excellent selectivity over α1-adrenoceptors (Ki > 1000 nM), 5-HT4 receptors, and benzodiazepine receptors. CSP-2503 inhibits cAMP increase in vitro and exhibits anxiolytic activity in vivo. CSP-2503 can be used for the research of anxiety-related disorders[1].

IC50 & Target[1]

5-HT1A Receptor

0.15 μM (EC50)

5-HT1A Receptor

4.1 nM (Ki)

5-HT2A Receptor

13.5 nM (Ki)

5-HT3 Receptor

8.9 nM (Ki)

5-HT4 Receptor

>10000 nM (Ki)

5-HT7 Receptor

100.9 nM (Ki)

α1-adrenergic receptor

>1000 nM (Ki)

serotonin transporter

976.3 nM (Ki)

benzodiazepine receptor

>10000 nM (Ki)

Dopamine D2 receptor

192.1 nM (Ki)

体外研究
(In Vitro)

CSP-2503 以剂量依赖性方式抑制 Forskolin (HY-15371) 诱导的 cAMP 升高,EC50 为 0.15 μM[1]

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

体内研究
(In Vivo)

CSP-2503 (10 mg/kg;皮下注射;单次给药) 在小鼠体内表现出抗焦虑活性[1]
CSP-2503 (2.5-20 mg/kg;皮下注射;单次给药) 在小鼠体内作为体树突 5-HT1A 受体激动剂发挥作用[1]

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

Animal Model: Mice[1]
Dosage: 10 mg/kg
Administration: s.c.; single dose
Result: Increased time spent in the lit area to 155.4 seconds compared to 83 seconds in vehicle-treated mice.
Increased time spent in the lit area by 87.2%.
Animal Model: Mice hypothermia model[1]
Dosage: 2.5, 5, 10, 20 mg/kg
Administration: s.c.; single dose
Result: Induced a dose-related decrease in rectal temperature.
Decreased the 5-HIAA/5-HT ratio in mouse hypothalamus.
分子量

378.48

Formula

C22H26N4O2

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.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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This equation is commonly abbreviated as: C1V1 = C2V2

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Help & FAQs
  • 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:
CSP-2503
目录号:
HY-180372
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