2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. TMU4142

TMU4142 是一种具有高 GoA 活性的选择性 5-HT1a 激动剂。TMU4142 的 Gi3 活性较弱，能够在不显著激活 DRN 区 5-HT1a 自身受体的情况下快速产生抗抑郁样效应或抑制血清素能神经元放电。TMU4142 在抑郁小鼠模型中显示出快速起效抗抑郁效果。TMU4142 可用于抗抑郁研究。

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TMU4142

TMU4142 Chemical Structure

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TMU4142 相关抗体

Top Publications Citing Use of Products

查看 5-HT Receptor 亚型特异性产品:

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TMU4142 is a selective 5-HT1a agonist with high GoA activity. TMU4142 has weak Gi3 activity, can elicit rapid antidepressant like effects without triggering significant activation of dorsal raphe nucleus (DRN) 5-HT1a R autoreceptors or serotonergic neuron firing. TMU4142 demonstrates fast-acting efficacy in mouse models of depression. TMU4142 can be used for antidepressants research[1].

IC50 & Target[1]

5-HT1A Receptor

 

体外研究
(In Vitro)

TMU4142 可激动 GoA 信号通路，对 Gi3 通路活性较弱，在与 5-HT1a 受体相关的 β-arrestin-2 通路上未显示出可检测到的活性；其在 5-HT1a 受体上表现出更高的效价，同时降低了对 β-肾上腺素能受体的活性[1]。

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

TMU4142 相关抗体:
体内研究
(In Vivo)

TMU4142 (0.3 或 1.5 mg/kg，腹腔注射) 具有 GoA 偏向性且 Gi3 活性极低，能够选择性激活主要位于突触后、与抗抑郁反应相关的 GoA 信号通路，同时避免由 Gi3 介导的突触前自身受体反馈抑制作用，从而在 C57BL/6 小鼠慢性束缚应激诱导的抑郁模型中维持 DRN 区 5-HT 的合成与释放[1]。

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

Animal Model: Chronic restraint stress (CRS)-induced depression model in male C57BL/6Jmice (8-12 weeks)[1]
Dosage: 0.3 or 1.5 mg/kg
Administration: i.p., once
Result: Significantly reduced the immobility time of CRS mice in the forced swim test (FST) 30min post-injection indicating an antidepressant-like effect.
Reversed CRS-induced depressive-like behaviors in mice at 1.5mg/kg.
Elicited significant antidepressant-like effects.
Exerted antidepressant-like effects in CRS mice through 5-HT1a R activation, as demonstrated by the blockade of the immobility-reducing effects in the FST and tail suspension test (TST) by the antagonist WAY 100635 (Y-10349).
Abolished the reduction in immobility time in both the FST and TST indicated that the antidepressant-like effects are mediated through the activation of 5-HTRA.
Significantly reduced the latency to feed in mice as early as 1 h after drug administration without affecting the home cage food intake.
Has acute effect in the NSF test was blocked by way-100635, suggesting that its action is mediated through5-HT1a Ractivation.
Did not alter DRN5-HT levels in CRS mice.
分子量

413.51

Formula

C23H31N3O4
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

TMU4142 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

TMU4142TMU 4142TMU-41425-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT1aGoAantidepressantDRN 5-HT1ARautoreceptorsInhibitorinhibitorinhibit

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目录号：
HY-179579
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