Clobenpropit
Clobenpropit structure
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Common Name | Clobenpropit | ||
|---|---|---|---|---|
| CAS Number | 145231-45-4 | Molecular Weight | 470.65300 | |
| Density | 1.31g/cm3 | Boiling Point | 551.3ºC at 760mmHg | |
| Molecular Formula | C14H19Br2ClN4S | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | 287.2ºC | |
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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 terminals (synaptosomes), we studied whether H3R activation m... |
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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 in the H(4)R binding pocket, D(3.32) and E(5.46), act as es... |
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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 the in vitro and in vivo effects of corticosterone (Cort) o... |
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The H4 histamine receptor agonist, clobenpropit, suppresses human cholangiocarcinoma progression by disruption of epithelial mesenchymal transition and tumor metastasis.
Hepatology 54(5) , 1718-28, (2011) Cholangiocarcinoma (CCA) is a biliary cancer arising from damaged bile ducts. Epithelial-mesenchymal transition (EMT) occurs as epithelial cells begin to resemble mesenchymal cells leading to increased invasion potential as the extracellular matrix (ECM) degr... |
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Attenuated expression of HRH4 in colorectal carcinomas: a potential influence on tumor growth and progression.
BMC Cancer 11 , 195:1-11, (2011) Earlier studies have reported the production of histamine in colorectal cancers (CRCs). The effect of histamine is largely determined locally by the histamine receptor expression pattern. Recent evidence suggests that the expression level of histamine recepto... |
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Electrophysiology-based analysis of human histamine H4receptor pharmacology using GIRK channel coupling inXenopusoocytes
Eur. J. Pharmacol. 591(1-3) , 52-8, (2008) The recently cloned histamine H 4 receptor is expressed predominantly in haematopoietic cells and has been found to modulate the function of mast cells, eosinophils, dendritic cells and T lymphocytes. It represents an attractive target for pharmacological int... |
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Efficient approaches to S-alkyl-N-alkylisothioureas: syntheses of histamine H3 antagonist clobenpropit and its analogues.
J. Org. Chem. 73(6) , 2096-104, (2008) S-Alkyl-N-alkylisothioureas were efficiently synthesized via synthetic approach (A) using 3-phenylpropionyl isothiocyanate (PPI). The utility of the approach was proved by the syntheses of clobenpropit, a potent histamine H(3) antagonist, and its analogues. A... |
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Role of H4 receptor in histamine-mediated responses in human melanoma.
Melanoma Res. 21(5) , 395-404, (2011) We have previously reported that histamine at micromolar concentrations reduces the proliferation of melanoma cell lines. It is also known that melanoma cells express histamine H1, H2, and H3 receptors. The aim of this study was to investigate the presence of... |
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Protective effects of histamine H3-receptor ligands in schizophrenic behaviors in experimental models
Pharmacol. Rep. 64(1) , 191-204, (2012) Schizophrenia (SCZ) afflicts around 1% of the world’s population with characteristic symptoms such as hallucinations, delusions, and cognitive disorders. Several experimental studies in the past have indicted brain histaminergic neuronal system involvement in... |
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Short photoperiod-induced decrease of histamine H3 receptors facilitates activation of hypothalamic neurons in the Siberian hamster.
Endocrinology 150(8) , 3655-63, (2009) Nonhibernating seasonal mammals have adapted to temporal changes in food availability through behavioral and physiological mechanisms to store food and energy during times of predictable plenty and conserve energy during predicted shortage. Little is known, h... |