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[(4-氯苯基)甲基]-脲基硫代酸-3-(1H-咪唑-4-基)丙酯

用途

氯苯丙胺是一种有效的组胺H3受体拮抗剂。氯苯丙胺减少多巴胺释放,增加下丘脑组胺水平。Clobenpropit表现出抗精神病药样活性。Clobenpropit对失血性休克大鼠产生复苏作用[1][2]。

名称

[ CAS 号 ]:
145231-45-4

[ 中文名 ]:
[(4-氯苯基)甲基]-脲基硫代酸-3-(1H-咪唑-4-基)丙酯

[ 英文名 ]:
Clobenpropit

[英文别名 ]:

生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 免疫及炎症 >> 组胺受体

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

[ 靶点 ]

H3 receptor

[体内研究]

氯苯丙胺(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型诱导的过度运动行为[1]。< br/＞氯苯丙胺(1、2、5μmoL/kg静脉注射) 对遭受失血性休克的大鼠产生复苏作用[2]。动物模型：150-200g,12周龄雄性wistar白化大鼠[1]剂量：15mg/kg给药：I.p。；结果：单剂量MK-801(0.2 mg/kg,i.p.)可显著降低MK-801诱导的过度运动活动,并减少MK-801诱发的多巴胺释放,下丘脑组胺水平进一步增加。动物模型：205-470g,成年雄性Wistar大鼠[2]剂量：1、2、5μmoL/kg(在6-羟基多巴胺(50 mg/kg(SC)连续3天后)给药：静脉注射结果：触发平均动脉压(MAP)(剂量2μmoL/kg)和心率(HR)(剂量1、2和5μmoL/kg。

[参考文献]

[1]. Mahmood D, et al. The Effect of Subchronic Dosing of Ciproxifan and Clobenpropit on Dopamine and Histamine Levels in Rats. J Exp Neurosci. 2015 Aug 31;9:73-80.

[2]. Wanot B, et al. Cardiovascular effects of H3 histamine receptor inverse agonist/ H4 histamine receptor agonist, clobenpropit, in hemorrhage-shocked rats. PLoS One. 2018 Aug 2;13(8):e0201519.

物理化学性质

[ 密度 ]:
1.31g/cm3

[ 沸点 ]:
551.3ºC at 760mmHg

[ 分子式 ]:
C₁₄H₁₉Br₂ClN₄S

[ 分子量 ]:
470.65300

[ 闪点 ]:
287.2ºC

[ 精确质量 ]:
467.93900

[ PSA ]:
89.86000

[ LogP ]:
5.86030

[ 蒸汽压 ]:
3.35E-12mmHg at 25°C

[ 折射率 ]:
1.645

安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

文献

Histamine H3 receptor activation counteracts adenosine A2A receptor-mediated enhancement of depolarization-evoked [3H]-GABA release from rat globus pallidus synaptosomes.

ACS Chem. Neurosci. 5(8) , 637-45, (2014)

High levels of histamine H3 receptors (H3Rs) are found in the globus pallidus (GP), a neuronal nucleus in the basal ganglia involved in the control of motor behavior. By using rat GP isolated nerve te...

Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.

J. Med. Chem. 54 , 8136-47, (2011)

The histamine H(4) receptor (H(4)R) is a G protein-coupled receptor (GPCR) that plays an important role in inflammation. Similar to the homologous histamine H(3) receptor (H(3)R), two acidic residues ...

Adipogenic and lipolytic effects of chronic glucocorticoid exposure.

Am. J. Physiol. Cell Physiol. 300 , C198-209, (2011)

Glucocorticoids have been proposed to be both adipogenic and lipolytic in action within adipose tissue, although it is unknown whether these actions can occur simultaneously. Here we investigate both ...

更多文献

[(4-氯苯基)甲基]-脲基硫代酸-3-(1H-咪唑-4-基)丙酯

用途

名称

生物活性

物理化学性质

安全信息

文献

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