2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. Robalzotan hydrochloride

Robalzotan hydrochloride  (Synonyms: NAD-​299 hydrochloride)

目录号: HY-10351A
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Robalzotan hydrochloride (NAD- 299 hydrochloride) 是一种有效的选择性 5-Hydroxytryptamine 1A (5-HT1A) 抑制剂。Robalzotan hydrochloride 增加 5-HT 细胞的放电率。Robalzotan hydrochloride 诱导 5-HT1A 受体占据。Robalzotan hydrochloride 具有研究中枢神经系统胆碱能缺陷的潜力。

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Robalzotan hydrochloride Chemical Structure

Robalzotan hydrochloride Chemical Structure

CAS No. : 184674-99-5

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10 mg ￥4536
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Robalzotan hydrochloride 相关抗体

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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

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生物活性

Robalzotan hydrochloride (NAD-​299 hydrochloride) is a potent and selective 5-Hydroxytryptamine 1A (5-HT1A) inhibitor. Robalzotan hydrochloride increases the firing rate of 5-HT cells. Robalzotan hydrochloride induces 5-HT1A receptor occupancy. Robalzotan hydrochloride has the potential for the research of a cholinergic deficit in the central -nervous system[1][2][3].

IC50 & Target[1]

5-HT1A Receptor

 

体内研究
(In Vivo)

Robalzotan hydrochloride (1-100 µg/kg；i.v.) 在大鼠体内以 5 µg/kg 显着增加此类神经元的活性，并逆转 citalopram (HY-121203) (300 µg/kg i.v.) 或 paroxetine (HY-122272) (100 µg/kg， i.v.) 对大鼠中缝背核 5-HT神经元活性的影响[1].
Robalzotan hydrochloride (5, 50 µg/kg；静脉注射) 提高 5-HT 细胞的放电率[1]。
Robalzotan hydrochloride (2-100 µg/kg; i.v.) 在猴子体内以剂量依赖性方式占据 5-HT1A 受体[2]。
Robalzotan hydrochloride (0.3；1 和 3 µmol/kg 皮下注射) 引起大鼠 FC 细胞外 ACh 水平的剂量依赖性增加[3]。

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

Animal Model: 300-600 g, male Sprague-Dawley rats (5-HT cells)[1]
Dosage: 1, 5, 12.5, 25, 50, 100 µg/kg
Administration: I.v.
Result: Significantly increased the activity of such neurons at 5 µg/kg, increasing doses of robalzotan 5-100 µg/kg or 50-400 mg/kg did not further affect the firing rate of 5-HT neurons.
Animal Model: 3-4 kg, cynomolgus monkeys[2]
Dosage: 2, 10, 20, 100 µg/kg
Administration: I.v.
Result: Occupied 5-HT1A receptors in a dose-dependent and saturable manner and he highest 5-HT1A receptor occupancy (70-80%) was attained after 100 μg/kg.
分子量

354.85

Formula

C18H24ClFN2O2
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

Robalzotan hydrochloride 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Robalzotan184674-99-5NAD-​2995-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptorfiring rateneurons5-HT cellsACh levelscholinergic deficitInhibitorinhibitorinhibit

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