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An extremely potent histamine H3 antagonist/inverse agonist (pA2=9.93). Also displays partial agonist activity at H4 receptors; induces eosinophil shape change with an EC50 of 3 nM.
Sold with the permission of SCI, Amsterdam
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 470.65. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.12 mL||10.62 mL||21.25 mL|
|5 mM||0.42 mL||2.12 mL||4.25 mL|
|10 mM||0.21 mL||1.06 mL||2.12 mL|
|50 mM||0.04 mL||0.21 mL||0.42 mL|
References are publications that support the biological activity of the product.
Buckland et al (2003) Histamine induces cytoskeletal changes in human eosinophils via the H4 receptor. Br.J.Pharmacol. 140 1117 PMID: 14530216
Liu et al (2001) Cloning and pharmacological characterization of a fourth histamine receptor (H4) expressed in bone marrow. Mol. Pharmacol. 59 420 PMID: 11179434
Yokoyama et al (1994) Clobenpropit (VUF-9153), a new histamine H3 receptor antagonist, inhibits electrically induced convulsions in mice. Eur.J.Pharmacol. 260 23 PMID: 7957622
Van der Goot et al (1992) Isothiourea analogues of histamine as potent agonists or antagonists of the histamine H3 receptor. Eur.J.Med.Chem. 27 511
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Keywords: Clobenpropit dihydrobromide, Clobenpropit dihydrobromide supplier, H4, partial, agonists, H3, antagonists, inverse, potent, Receptors, Histamine, histaminergic, VUF9153, VUF, 9153, 0752, Tocris Bioscience
4 Citations for Clobenpropit dihydrobromide
Citations are publications that use Tocris products. Selected citations for Clobenpropit dihydrobromide include:
Hedegaard et al (2012) Molecular pharmacology of human NMDA receptors. Neurochem Int 61 601 PMID: 22197913
Alkan et al (2015) Histidine Decarboxylase Deficiency Prevents Autoimmune Diabetes in NOD Mice. J Immunol 2015 965056 PMID: 26090474
Flamand et al (2004) Histamine-induced inhibition of leukotriene biosynthesis in human neutrophils: involvement of the H2 receptor and cAMP. Br J Pharmacol 141 552 PMID: 14744809
Femenia et al (2015) Hippocampal-Dependent Antidepressant Action of the H3 Receptor Antagonist Clobenpropit in a Rat Model of Depression. Int J Neuropsychopharmacol 18 PMID: 25762718
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Literature in this Area
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Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.