2. Neuronal Signaling
  3. Sigma Receptor
  4. σ1 Receptor antagonist 4

σ1 Receptor antagonist 4 (compound TC1) 是一种选择性 sigma1 (σ1) 受体拮抗剂，Ki 为 10 nM。σ1 Receptor antagonist 4 对 σ2 受体（Ki 为 370 nM）的活性较弱，对多巴胺 (DAT)、血清素 (SERT) 和去甲肾上腺素 (NET) 转运体无活性。

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σ1 Receptor antagonist 4 Chemical Structure

σ1 Receptor antagonist 4 Chemical Structure

CAS No. : 362512-81-0

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σ1 Receptor antagonist 4 相关抗体

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Sigma 1 Receptor Sigma 2 Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

σ1 Receptor antagonist 4 (compound TC1) is a selective sigma1 (σ1) receptor antagonist with a Ki of 10 nM. σ1 Receptor antagonist 4 is weakly active at σ2 receptor (Ki of 370 nM) and has no activity at dopamine (DAT), serotonin (SERT), and norepinephrine (NET) transporters[1].

IC50 & Target[1]

σ1R

10 nM (Ki)

σ2

370 nM (Ki)

体内研究
(In Vivo)

σ1 Receptor antagonist 4（compound TC1; 3-100 mg/kg; 腹腔注射，单次）可减弱​​ 20 mg/kg 可卡因的刺激性运动效应，半数最大抑制活性 (ID50) 为 38.6 mg/kg[1]。

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

Animal Model: Male Swiss-Webster mice (Hsd:ND4, aged 2-3 month) injected with Cocaine[1]
Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg
Administration: i.p.; once
Result: Attenuated the stimulatory locomotor effect of 20 mg/kg Cocaine.
分子量

297.37

Formula

C19H20FNO
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

σ1 Receptor antagonist 4 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

σ1 Receptor antagonist 4362512-81-0Sigma Receptorσ1 receptor antagonistInhibitorinhibitorinhibit

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σ1 Receptor antagonist 4
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