2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. CP-809101

CP-809101 是一种强效的，高选择性的 5-HT2C 受体激动剂，其对人 5HT2C, 5HT2B 和 5HT2A 受体的 pEC50 值分别为 9.96, 7.19 和 6.81 M。CP-809101 能抑制大鼠的条件回避反应，以及 phencyclidine hydrochloride 和 d-amphetamine 诱导的多动症，还能减少大鼠对食物和尼古丁的依赖。CP-809101 可用于抗精神病以及尼古丁依赖的研究。

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CP-809101 Chemical Structure

CP-809101 Chemical Structure

CAS No. : 479683-64-2

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CP-809101 的其他形式现货产品:

Other Forms of CP-809101:

CP-809101 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

查看 5-HT Receptor 亚型特异性产品:

查看所有亚型
5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CP-809101 is a potent and highly selective 5-HT2C receptor agonist, with pEC50s of 9.96, 7.19 and 6.81 M for human 5HT2C, 5HT2B and 5HT2A receptor. CP-809101 inhibits conditioned avoidance responding in rats and antagonizes both PCP (phencyclidine hydrochloride)- and d-amphetamine-induced hyperactivity. CP-809101 also reduces food and nicotine dependence in rats, can be used in studies of antipsychotic and nicotine dependence[1][2].

IC50 & Target

5-HT2C Receptor

9.96 (pEC50)

5-HT2B Receptor

7.19 (pEC50)

5-HT2A Receptor

6.81 (pEC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 EC50
0.0019 μM
Compound: CP 809101
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
[PMID: 23301527]
HEK293 EC50
0.0081 μM
Compound: CP 809101
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
[PMID: 23301527]
HEK293 EC50
0.076 μM
Compound: CP 809101
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
[PMID: 23301527]
HEK293 EC50
0.14 μM
Compound: CP 809101
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
[PMID: 23301527]
体内研究
(In Vivo)

CP-809101 (0.1-56 mg/kg; s.c.; single) inhibits the conditioned avoidance response of rats in a dose-dependent manner[1].
CP-809101 (0.56, 1.78, 5.6, 17.8 mg/kg; s.c.; single) antagonizes PCP (phencyclidine hydrochloride)-induced and d-amphetamine-induced hyperactivity (the latter in a dose-dependent manner)[1].
CP-809101 (0.56, 1.78, 5.6, 17.8 mg/kg; s.c.; single) dose-dependently decreases spontaneous locomotor activity with an ED50 value of 2.2 mg/kg[1].
CP-809101 (0.3, 1, 3 mg/kg; s.c.; single) reduces responding for both nicotine and food and blocked the discriminative stimulus properties of nicotine[2].

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

Animal Model: Male CF rats (conditioned avoidance responding (CAR) model)[1].
Dosage: 0.1-56 mg/kg
Administration: Subcutaneous injection; single.
Result: Resulted in a dose-dependent inhibition of the conditioned avoidance response with an ID50 value of 4.8 mg/kg.
Animal Model: Male CD rats (PCP or d-amphetamine-induced hyperactivity model)[1].
Dosage: 0.56, 1.78, 5.6, 17.8 mg/kg
Administration: Subcutaneous injection; single.
Result: Antagonized PCP-induced hyperactivity, with an ED50 value of 2.4 mg/kg.
Antagonized d-amphetamine-induced hyperactivity, with an ED50 value of 2.7 mg/kg, and in a dose-dependent manner.
Animal Model: Male CD rats (spontaneous locomotor model)[1].
Dosage: 0.56, 1.78, 5.6, 17.8 mg/kg
Administration: Subcutaneous injection; single.
Result: Inhibited spontaneous locomotor activity in a dose-dependent manner (ED50=2.7 mg/kg).
Animal Model: Adult male Sprague-Dawley rats (280-400 g)[2].
Dosage: 0.3, 1, 3 mg/kg
Administration: Subcutaneous injection; single.
Result: Produced a dose-related decrease in responding for food and nicotine self-administration in rats.
分子量

304.77

Formula

C15H17ClN4O
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

CP-809101 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

CP-809101479683-64-2CP809101CP 8091015-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptorantipsychoticconditioned avoidance respondinghyperactivitynicotine dependencenicotineInhibitorinhibitorinhibit

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