2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. Clobenpropit

Clobenpropit 是一种有效的组胺 H3 受体 (histamine H3-receptor) 拮抗剂。Clobenpropit 减少多巴胺释放并增加下丘脑中的组胺水平。Clobenpropit 表现出类似抗精神病药的活性。Clobenpropit 对遭受失血性休克的大鼠产生复苏作用。

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 Clobenpropit dihydrobromide 通常具有更好的水溶性和稳定性。

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Clobenpropit Chemical Structure

Clobenpropit Chemical Structure

CAS No. : 145231-45-4

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Clobenpropit 的其他形式现货产品:

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Clobenpropit 相关抗体

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H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Clobenpropit is a potent histamine H3-receptor antagonist. Clobenpropit decreases dopamine release and increases histamine levels in the hypothalamus. Clobenpropit shows antipsychotic-like activities. Clobenpropit causes a resuscitating effect in rats subjected to the hemorrhagic shock[1][2].

IC50 & Target[1]

H3 receptor

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 EC50
1.7 nM
Compound: clobenpropit
Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay
Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay
[PMID: 19553110]
HT-1080 IC50
1 nM
Compound: Clobenpropit
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
[PMID: 20833043]
HT-1080 IC50
1 nM
Compound: Clobenpropit
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
[PMID: 20833043]
体内研究
(In Vivo)

Clobenpropit (15 mg/kg；腹腔注射；每天一次，持续 7 天) 可抵消 MK-801 (HY-15084B) 对多巴胺和组胺水平的调节作用，并防止 MK-801 诱导的过度运动行为[1]。< br/> Clobenpropit (1、2、5 μmoL/kg；静脉注射) 对遭受失血性休克的大鼠产生复苏作用[2]。

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

Animal Model: 150-200g, 12-week-old male wistar albino rats[1]
Dosage: 15 mg/kg
Administration: I.p.; once daily for 7 days
Result: Exhibited a significant reduction of hyperlocomotor activities induced by a single-dose administration of MK-801 (0.2 mg/kg, i.p.), and reduced the MK-801-induced dopamine release, exhibited further increase in histamine levels in the hypothalamus.
Animal Model: 205-470g, adult male Wistar rats[2]
Dosage: 1, 2, 5 μmoL/kg (after 6-hydroxydopamine (50 mg/kg (SC) for 3 consecutive days)
Administration: I.v.
Result: Triggered a statistically significant increase of mean arterial pressure (MAP) (dose 2 μmol/kg) and heart rate (HR) (doses of 1, 2, 5 μmol/kg).
分子量

308.83

Formula

C14H17ClN4S
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

Clobenpropit 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

Clobenpropit145231-45-4Histamine Receptordopaminehistamineantipsychotic-likehemorrhagic shockMAPHRInhibitorinhibitorinhibit

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目录号：
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