2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. CP-283097

CP-283097 是一种口服有效的、构象受限的、NR2B 亚型选择性的 NMDA 受体拮抗剂。CP-283097 能有效竞争性抑制 [³H]CP-101,606 与大鼠脑膜的结合，IC50 值为 18 nM。CP-283097 对 NR2B 受体介导的电流几乎完全抑制 (IC50 = 206 nM)，而对 NR2A 或 NR2C 受体的抑制作用很弱。CP-283097 在动物模型中表现出优异的中枢神经系统渗透性和体内疗效。CP-283097 可用于研究与 NMDA 受体过度激活相关的神经系统疾病。

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CP-283097

CP-283097 Chemical Structure

CAS No. : 138047-56-0

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CP-283097 相关抗体

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AMPA Receptor NMDA Receptor Kainate Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CP-283097 is an orally active and conformationally restricted and NR2B subtype-selective NMDA antagonist. CP-283097 efficiently competitively inhibits the binding of [³H]CP-101,606 to the rat meninges, with an IC50 value of 18 nM. CP-283097 exhibits nearly complete inhibition of the current mediated by the NR2B receptor (IC50 = 206 nM), while the inhibitory effect on the NR2A or NR2C receptors is very weak. CP-283097 demonstrates excellent central nervous system permeability and in vivo efficacy in animal models. CP-283097 can be used for neurological diseases related to excessive activation of NMDA receptors[1].

体外研究
(In Vitro)

CP-283097 对谷氨酸诱导的海马神经元毒性的抑制作用 IC50 为 4 nM[1]。

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

CP-283097 相关抗体:
体内研究
(In Vivo)

CP-283097 (皮下注射和口服，单次给药) 在 Haloperidol (HY-14538) 诱导的僵直模型大鼠中抑制 NMDA 受体，其 ED50 分别为 0.3 mg/kg 和 1.2 mg/kg[1]。
CP-283097 (1-15 mg/kg，静脉注射，单次给药) 抑制 NMDA 诱导的 c-Fos 表达，在小鼠中 ED50 为 4 mg/kg[1]。
CP-283097 (0.2-2 mg/kg，静脉注射，单次给药) 可有效抑制大鼠电刺激诱发的病理性皮层传播活动 (CSD)[1]。

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

Animal Model: Cortical spreading depression model established in rats[1]
Dosage: 0.2, 0.6 and 2 mg/kg bolus + 0.2, 0.6 and 2 mg/kg infusion
Administration: Intravenous injection (i.v.), single dose
Result: Dose-dependently inhibited CSD propagation.
分子量

355.43

Formula

C21H25NO4
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-283097 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)

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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)
× = ×
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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.

Keywords:

CP-283097138047-56-0CP283097CP 283097iGluRIonotropic glutamate receptorsneuroprotective potencycortical spreading depression (CSD) inhibitionoral bioavailabilitystereochemical preference crossoverInhibitorinhibitorinhibit

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