2. Neuronal Signaling GPCR/G Protein
  3. Serotonin Transporter 5-HT Receptor
  4. LY 367265

LY 367265 是一种 5-羟色胺转运体 (SERT) 抑制剂 (IC50 = 3.1 nM) 和 5-HT₂A 受体 (5-HT₂A receptor) (Ki = 0.81 nM) 拮抗剂。LY 367265 对去甲肾上腺素转运体 (NET) 抑制活性极弱 (IC₅₀ > 1000 nM)；对 5-HT₁B (Kᵢ = 490 nM)、5-HT₁D (Kᵢ = 81 nM) 等亚型亲和力低，显示高选择性。LY367265 浓度依赖性增强 [³H]5-HT 外流 (EC50 = 250 nM)。LY 367265 拮抗 Sumatriptan (HY-B0121B) 的收缩反应，表明其对 5-HT₁D 样受体具有功能性拮抗活性。LY 367265 可用于研究焦虑障碍、创伤后应激障碍等疾病。

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LY 367265

LY 367265 Chemical Structure

CAS No. : 210751-39-6

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LY 367265 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

LY 367265 is a 5-hydroxytryptamine transporter (SERT) inhibitor (IC₅₀ = 3.1 nM) and a 5-HT₂A receptor antagonist (Kᵢ = 0.81 nM). LY 367265 has the inhibitory activity on the norepinephrine transporter (NET) of extremely weak (IC₅₀ > 1000 nM); it has low affinity for subtypes such as 5-HT₁B (Kᵢ = 490 nM) and 5-HT₁D (Kᵢ = 81 nM), showing high selectivity. LY 367265 concentration-dependently enhances of [³H]5-HT efflux (EC₅₀ = 250 nM). LY 367265 antagonizes the contraction response of Sumatriptan (HY-B0121B), indicating its functional antagonistic activity on 5-HT₁D-like receptors. LY 367265 can be used for the study of diseases such as anxiety disorders and post-traumatic stress disorder[1].
IC50 & Target[1]

5-HT2A Receptor

0.81 nM (Ki)

5-HT1B Receptor

490 nM (Ki)

5-HT1D Receptor

81 nM (Ki)

分子量

452.54

Formula

C24H25FN4O2S
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

LY 367265 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:

LY 367265210751-39-6LY367265LY-367265Serotonin Transporter5-HT Receptor5-HTTSERTSLC6A4Serotonin Receptor5-hydroxytryptamine Receptor5-HT transporter inhibitor5-HT2A receptor antagonistdual-acting antidepressantnefazodone comparisonserotonin releasesynaptic mechanismpreclinical pharmacologyside effect reductiondepressive disordersInhibitorinhibitorinhibit

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产品名称：
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HY-156807
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