2. Neuronal Signaling GPCR/G Protein
  3. Sigma Receptor 5-HT Receptor
  4. OPC-14523 free base

OPC-14523 free base 是一种具有口服活性的 sigma 和 5-HT1A 受体激动剂，对 sigma 受体 (σ1/2 IC50=47/56 nM)、5-HT1A 受体 (IC50=2.3 nM) 和 5-HT 转运体 (IC50=80 nM) 具有高度亲和力。OPC-14523 free base 显示抗抑郁药样活性。

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 OPC-14523 hydrochloride 通常具有更好的水溶性和稳定性。

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OPC-14523 free base Chemical Structure

OPC-14523 free base Chemical Structure

CAS No. : 145969-30-8

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OPC-14523 free base 的其他形式现货产品:

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Other Forms of OPC-14523 free base:

OPC-14523 free base 相关抗体

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查看 Sigma Receptor 亚型特异性产品:

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Sigma 1 Receptor Sigma 2 Receptor

查看 5-HT Receptor 亚型特异性产品:

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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

OPC-14523 free base is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 free base shows antidepressant-like activity[1][2].

IC50 & Target[1]

5-HT1A Receptor

2.3 nM (IC50)

sigma 1

47 nM (IC50)

sigma 2

56 nM (IC50)

体内研究
(In Vivo)

OPC-14523 free base (0.3-100 mg/kg; p.o.; daily for 0, 2, 4, 7 days) produces a marked antidepressant-like effect in the forced swimming test (FST) with rats and mice without affecting the general locomotor activity[1].

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

Animal Model: Wistar strain of rats (140-245 g)[1]
Dosage: 0.3-100 mg/kg
Administration: P.o.; daily for 0, 2, 4, 7 days
Result: A single doses of 1 mg/kg and higher of OPC-14523 reduced immobility time in the FST with an ED50 value of 27 mg/kg. The ED50 value for OPC-14523 on day 7 was 18 mg/kg.
Animal Model: ICR strain of mice (25-45 g)[1]
Dosage: 0.3-100 mg/kg
Administration: P.o.; daily for 0, 2, 4, 7 days
Result: A single oral dose of OPC-14523 produced a marked reduction in immobility time during the FST at oral doses of 1 mg/kg and higher, with an ED50 value of 20 mg/kg. The potency of OPC-14523 in decreasing immobility time was greater after treatment for seven consecutive days, producing an ED50 value of 2 mg/kg.
分子量

413.94

Formula

C23H28ClN3O2
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

OPC-14523 free base 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

OPC-14523145969-30-8OPC14523OPC 14523Sigma Receptor5-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorantidepressantaffinityreuptakeimmobilityswimmingsubtypeInhibitorinhibitorinhibit

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