2. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein
  3. Monoamine Transporter Serotonin Transporter Dopamine Transporter 5-HT Receptor
  4. 6-APDB

6-APDB 是一类单胺类递质释放剂与单胺转运体 (Monoamine Transporter) 调节剂，对人源单胺转运体具有选择性作用，对 5-HT2 家族受体存在部分激动作用。6-APDB 对 NET 的 IC50 为 0.56 μM、Ki 为 18 μM；对 SERT 的 IC50 为 2.3 μM、Ki 为 23 μM；对 DAT 的 IC50 为 33 μM、Ki＞30 μM。同时，6-APDB 对大鼠及小鼠 TAAR1 的 Ki 分别为 1.0 μM 和 0.21 μM。6-APDB 可抑制去甲肾上腺素和 5-HT 再摄取、介导三类单胺递质释放，在小鼠中呈现剂量依赖性的双向运动效应，且可完全替代 MDMA 的辨别刺激效应。6-APDB 在高浓度下无明显细胞毒性，具有致共情的精神活性、潜在致幻作用及与间歇性滥用相关的行为效应。

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6-APDB

6-APDB Chemical Structure

CAS No. : 152623-93-3

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Other Forms of 6-APDB:

6-APDB 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-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

6-APDB is a class of monoamine neurotransmitter releaser and Monoamine Transporter modulator that exerts selective effects on human monoamine transporters and acts as a partial agonist at 5-HT2 family receptors. For NET, 6-APDB has an IC50 of 0.56 μM and a Ki of 18 μM; for SERT, it has an IC50 of 2.3 μM and a Ki of 23 μM; for DAT, it has an IC50 of 33 μM and a Ki of >30 μM, and affinity for rat and mouse TAAR1, with Ki values of 1.0 μM and 0.21 μM, respectively. 6-APDB inhibits norepinephrine and 5-HT reuptake, mediates the release of three types of monoamine neurotransmitters, shows a dose-dependent biphasic locomotor effect in mice, and fully substitutes the discriminative stimulus effect of MDMA. 6-APDB shows no significant cytotoxicity at high concentrations, and possesses empathogenic psychoactivity, potential hallucinogenic effects, and behavioral effects associated with intermittent abuse[1][2].

IC50 & Target

human 5-HT2B Receptor

 

体外研究
(In Vitro)

6-APDB (1 nM-100 μM; 10 min) 可抑制表达 NET、DAT 和 SERT 的 HEK 293 细胞对单胺类物质的摄取，其中对 NET 的效力最高，对 SERT 的效力中等，对 DAT 的效力最低，最终呈现出较低的 DAT:SERT 比值，表明其具有偏好性的 5-羟色胺能活性[1]。
6-APDB (100 μM; 45 min or 15 min) 可诱导表达单胺转运体的 HEK 293 细胞经转运体介导释放去甲肾上腺素、多巴胺和 5-羟色胺[1]。
6-APDB (1 nM-100 μM; 10 min) 在 HEK 293 细胞中可作为人源 5-HT2A 受体的低效价部分激动剂，以及人源 5-HT2B 受体的高效价部分激动剂[1]。

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

6-APDB 相关抗体:

ELISA Assay[1]

Cell Line: HEK 293 cells
Concentration: 100 μM
Incubation Time: 45 min for NA release; 15 min for dopamine, 5-HT release
Result: Induced by a high concentration of the compound (100 μM) after preloading the transporter-transfected cells with the respective radiolabelled monoamine.
Induced transporter-mediated release of noradrenaline, dopamine, and 5-HT similarly to methamphetamine and MDMA.
体内研究
(In Vivo)

6-APDB (1-25 mg/kg; i.p.; 单剂量) 可对雄性 Swiss-Webster 小鼠产生剂量依赖性的运动兴奋性，其 ED50 为 2.80 mg/kg，且高剂量会先诱发活动抑制，随后出现延迟性兴奋[2]。
在雄性 Sprague‑Dawley 大鼠药物辨别实验中，6‑APDB (0.25–2.5 mg/kg，腹腔注射，单剂量，测试前预处理 40 min) 对甲基苯丙胺、可卡因和 DOM 仅表现出部分替代作用，且高剂量可抑制反应率；而 (0.05-1 mg/kg) 可完全替代 MDMA 的辨别刺激效应，在经过训练的雄性 Sprague-Dawley 大鼠中其 ED50 为 0.21 mg/kg[2]。

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

Animal Model: Sprague-Dawley (male, 320-350 g, trained to discriminate methamphetamine from vehicle)[2]
Dosage: 0.25, 0.5, 1, 2.5 mg/kg
Administration: i.p.; single dose; 40 minutes pre-test
Result: At 1 mg/kg, produced discrimination responses of 33±21% for methamphetamine, 53±21% for cocaine, and 67±21% for DOM, respectively.
At 2.5 mg/kg, almost completely inhibited the responses.
分子量

177.24

Formula

C11H15NO
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

6-APDB 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)

质量   浓度   体积   分子量 *
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The dilution calculator equation

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)
× = ×
C1   V1   C2   V2
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:

6-APDB152623-93-3Monoamine TransporterSerotonin TransporterDopamine Transporter5-HT Receptor5-HTTSERTSLC6A4DATSLC6A3Serotonin Receptor5-hydroxytryptamine Receptorrat TA1 receptorserotoninhuman SERThuman NEThuman 5-HT2β receptorshuman DATmouse TA1 receptornoradrenalinehuman 5-HT2? receptorsdopamineInhibitorinhibitorinhibit

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