2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. Fipamezole

Fipamezole  (Synonyms: MPV 1730; JP-1730)

目录号: HY-106444
产品使用指南

摩尔计算器

Fipamezole (MPV 1730; JP-1730) 是一种有效的且具有口服活性的 α2-肾上腺素受体 (α2-adrenergic receptor) 拮抗剂，对人类 α2A、α2B 和 α2C 受体的 Ki 值分别为 9.2 nM、17 nM 和 55 nM。Fipamezole 是一种抗运动障碍剂，可用于研究帕金森病。

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Fipamezole Chemical Structure

Fipamezole Chemical Structure

CAS No. : 150586-58-6

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Fipamezole 相关抗体

Top Publications Citing Use of Products

查看 Adrenergic Receptor 亚型特异性产品:

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α adrenergic receptor β adrenergic receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Fipamezole (MPV 1730; JP-1730) is a potent and orally active α2-adrenergic receptor antagonist with Ki values of 9.2 nM, 17 nM, and 55 nM for human α2A, α2B, and α2C, receptors, respectively. Fipamezole is an anti-dyskinetic agent, and can be used for the study of Parkinson's disease[1].

IC50 & Target[1]

human α2A-adrenoceptor

9.2 nM (Ki)

human α2B-adrenoceptor

17 nM (Ki)

human α2C-adrenoceptor

55 nM (Ki)

体外研究
(In Vitro)

在功能测定中，Fipamezole (JP-1730) 的强效拮抗剂特性表现为它能够降低肾上腺素诱导的 35S-GTPγS 结合，KB 值分别为 8.4 nM、16 nM、4.7 nM（在人类 α2A、α2B 和 α2C 受体上）。Fipamezole 对组胺 H1 和 H3 受体以及血清素 (5-HT) 转运体也具有中等亲和力（IC50 为 100 nM-1 μM）[1]。

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

Fipamezole 相关抗体:
体内研究
(In Vivo)

在 MPTP 损伤的狨猴中，Fipamezole (1-10 mg/kg；口服；单次) 显著减轻了 L-DOPA (HY-N0304) 引起的运动障碍，同时又不影响 L-DOPA 的抗帕金森病作用[1]。

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

Animal Model: Adult common marmosets (Callithrix jacchus, 300-345 g) injected with MPTP hydrochloride (2 mg/kg) and L-DOPA (8 mg/kg)[1]
Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg
Administration: po; once
Result: Significantly reduced L-DOPA-induced dyskinesia.
分子量

230.28

Formula

C14H15FN2
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

Fipamezole 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 *
= × ×

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:

Fipamezole150586-58-6MPV 1730 JP-1730MPV1730MPV-1730JP1730JP 1730JP-1730Adrenergic ReceptorBeta Receptorα2-adrenergic receptor antagonistanti-dyskinetic agentParkinson's diseaseInhibitorinhibitorinhibit

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