2. Neuronal Signaling GPCR/G Protein
  3. Serotonin Transporter 5-HT Receptor
  4. Wf-516

Wf-516 是一种 5-HT reuptake 的抑制剂，同时为 5-HT1A 和 5-HT2A 受体拮抗剂，对人体 5-HT1A 和 5-HT2A 受体的 Ki 值分别为 5 nM 和 40 nM，具有抗抑郁作用。

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Wf-516 Chemical Structure

Wf-516 Chemical Structure

CAS No. : 310392-94-0

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Other Forms of Wf-516:

Wf-516 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

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Wf-516 is an inhibitor of 5-HT reuptake, and an antagonist of 5-HT1A and 5-HT2A receptors, with Ki of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively, and has potent antidepressant activity.

IC50 & Target[1]

5-HT1A Receptor

5 nM (Ki)

5-HT2A Receptor

40 nM (Ki)

体外研究
(In Vitro)

Wf-516 shows high affinity for 5-HT1A receptors in the hippocampus and raphe nucleus of rats with Ki of 8.1 nM and 7.9 nM, respectively[2].

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

Wf-516 相关抗体:
体内研究
(In Vivo)

Wf-516 (0.5 mg/kg, i.v.) does not induce any change in the firing activity of 5-HT neurons, but significantly blocks the inhibitory effect of 8-OHDPAT (a 5-HT autoreceptor agonist) by 70%. A full dose-response relationship between the suppression of DRN firing activity and different doses of LSD shows a significant fourfold shift to the right in the Wf-516 pretreated rats (ED50 = 32.4 ± 1.0 μg/kg) as compared to controls (ED50 = 7.5 ± 1.2 μg/kg). After intravenous administration of successive doses of 1.25 mg/kg of Wf-516 (up to 10 mg/kg), the effect of microiontophoretically applied 5-HT is prolonged and reaches statistical significance at 7.5 mg/kg. At this dose, the RT50 value is increased by 53% and, by 75% at the highest dose of 10 mg/kg of Wf-516 used[1]. Oral administration of 30 mg/kg Wf-516 to these 5,7-DHT-treated rats induces a significant decrease of BPND in the hippocampus as compared with baseline, but no additional reduction of BPND is observed in the raphe nucleus. Oral ED50 values for Wf-516 in the hippocampus and raphe nucleus are 5.3 mg/kg and 4.2 mg/kg, respectively[2].

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

502.39

Formula

C25H25Cl2N3O4
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
Animal Administration
[2]

A series of 6 and 5 dynamic PET scans is performed for each rat approximately 5 h and 30 min after oral and intraperitoneal pretreatments with graded doses of Wf-516 (vehicle only, 1, 3, 10, 30 and 100 mg/kg) and pindolol (vehicle only, 1, 3, 10 and 30 mg/kg), respectively. Scans for the same individual rat receiving Wf-516 (n = 4) and pindolol (n = 3) are conducted more than 2 weeks and 1 week apart, respectively. PET imaging is also carried out for rats receiving oral administration of 30 mg/kg fluvoxamine dissolved in 0.5%HPMC 30 min before pindolol treatment in order to investigate the effects of fluvoxamine-induced increase of endogenous 5-HTs on the measurements of 5-HT1A receptor occupancies.

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

Wf-516 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

Wf-516310392-94-0Wf516Wf 516Serotonin Transporter5-HT Receptor5-HTTSERTSLC6A4Serotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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产品名称：
Wf-516
目录号：
HY-19417A
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