1. Others Neuronal Signaling Membrane Transporter/Ion Channel
  2. Insecticide GABA Receptor Chloride Channel
  3. Leptophos oxon

Leptophos oxon ,即溴苯磷的代谢产物,是一种 GABAA 受体氯离子通道抑制剂,其 IC50 值为 89.6 μM。Leptophos oxon 可抑制 GABA 诱导的氯离子内流,结合 GABAA 受体相关的 TBPS 位点,并抑制 TBPS 与电压依赖性氯离子通道的结合。Leptophos oxon 是一种杀虫剂,可用于神经系统疾病的研究。

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Leptophos oxon

Leptophos oxon Chemical Structure

CAS No. : 25006-32-0

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  • 生物活性

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  • 参考文献

生物活性

Leptophos oxon, a metabolite of leptophos, is a GABAA receptor chloride channel inhibitor with an IC50 values of 89.6 μM. Leptophos oxon inhibits GABA-induced chloride influx, binds to GABAA receptor-associated TBPS sites, and inhibits TBPS binding to voltage-dependent chloride channels. Leptophos oxon is a insecticide. Leptophos oxon can be used for the research of neurological disease[2].

IC50 & Target[1]

GABAA

 

体外研究
(In Vitro)

Leptophos oxon (预处理 15 分钟) 可抑制大鼠脑膜微粒体中 GABAa 受体介导的 36Cl- 内流,其 IC50 为 89.6 ± 30.4 μM[2]
Leptophos oxon (90 分钟) 可抑制 [35S]TBPS 与大鼠脑内 GABAa 受体的结合,其 IC50 为 13.4 ± 0.1 μM[2]
Leptophos oxon (60 分钟) 可抑制 [35S]TBPS 与加州电鳐 (Torpedo californica) 发电器官膜上电压依赖性 Cl- 通道的结合,其 IC50 为 2.4 ± 0.1 μM,最大抑制率可达对照组的 70-80%[2]

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

体内研究
(In Vivo)

Leptophos oxon (25 mg/kg 的硫磷;口服给药) 是雌性瑞士小鼠体内对硫磷的一种次要代谢物,占回收总放射性的比例不足 1%,且仅经粪便排泄[1]

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

Animal Model: Swiss mice (female, 35-40 g)[1]
Dosage: Detected as metabolite of 25 mg/kg leptophos
Administration: p.o. (leptophos administration)
Result: Was detected only in mouse feces, accounting for 0.9% of total recovered radioactivity from phenoxy-labeled leptophos treatment.
Was detected only in mouse feces, accounting for 0.4% of total recovered radioactivity from phenyl-labeled leptophos treatment.
分子量

396.00

Formula

C13H10BrCl2O3P

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
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Leptophos oxon
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