2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. 5-HT1AR agonist 1

5-HT1AR agonist 1 (Compound A3) 呈现出相对平衡的多靶点活性特征，包括 5-HT1AR 激动剂 (EC50 = 34 nM)、SERT 再摄取抑制剂 (IC50 = 12 nM)、 NET 再摄取抑制剂 (IC50 = 78 nM) 和 DAT 再摄取抑制剂 (IC50 = 135 nM)。5-HT1AR agonist 1 表现出显著的抗抑郁效果以及优异的生物利用度和低清除率，有望用于抗抑郁药物领域的研究sup>[1]。

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5-HT1AR agonist 1 Chemical Structure

5-HT1AR agonist 1 Chemical Structure

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5-HT1AR agonist 1 相关抗体

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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

5-HT1AR agonist 1 (Compound A3) emerges as a relatively balanced multi-target activity profile, including 5-HT1AR agonist with an EC50 value of 34 nM, SERT reuptake ihibitor (IC50 =12 nM), NET reuptake inhibitor (IC50 =78 nM) and DAT reuptake inhibitor (IC50 =135 nM). 5-HT1AR agonist 1 performs significant antidepressant effects and exhibits excellent bioavailability and low clearance in mice, which is promising for research in the field of antidepressant drugs[1].
IC50 & Target[1]

SERT

12 nM (IC50)

NET

78 nM (IC50)

DAT

135 nM (IC50)

体内研究
(In Vivo)

5-HT1AR agonist 1 (2.5 MG/ KG, I.V. and 10 MG / KG, P.O.) 在小鼠中表现出优秀的口服生物利用度和低清除率[1]。
5-HT1AR agonist 1 (30 MG/KG, i.p., 30 min) 在小鼠强迫游泳测试中展示了强大的抗抑郁潜力，类似于 Vilazodone (HY-14262) 的效果[1]。

5-HT1AR agonist 1在ICR小鼠体内药动学参数[1]

药代动力学分析[1]

Route Dose (mg/kg) Tmax (h) Cmax (ng/mL) AUClast (ng·h/mL) T1/2 (h) CL (mL/min/kg) Vd (L/kg) F (%)
A3 PO. 2.07 ± 0.15 0.42 ± 0.08 4980 ± 1590 16913 ± 2451 / / 147 %
10 mg/kg
IV. 2.64 ± 0.50 0.08 ± 0.00 2633 ± 104 2842 ± 142 14.62 ± 0.78 3.38 ± 0.79
10 mg/kg

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

Animal Model: Male ICR mice
Dosage: 2.5 MG/ KG, I.V. and 10 MG / KG, P.O.
Administration: I.V. and P.O., a single dose
Result: Showed excellent oral bioavailability in mice[1]
Animal Model: C57 mice
Dosage: 30 MG/KG
Administration: i.p., a single dose
Result: Significantly reduced immobility time in the forced swimming test in mice, similar to the effect of Vilazodone (HY-14262)[1]
分子量

418.49

Formula

C24H26N4O3
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

5-HT1AR agonist 1 相关分类

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The molarity calculator equation

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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:

5-HT1AR agonist 15-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT1AR agonismSERT reuptake ihibitionNET reuptake inhibitionDAT reuptake inhibitionantidepressant effectsdepressant deseaseInhibitorinhibitorinhibit

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