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. Also available as part of the Histamine H3 Receptor Tocriset™.
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.
All Tocris products are intended for laboratory research use only.
|Solubility||Soluble to 100 mM in water|
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 solvent 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 products' biological activity.
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
If you know of a relevant reference for Clobenpropit dihydrobromide, please let us know.
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Keywords: Clobenpropit dihydrobromide, supplier, H4, partial, agonists, H3, antagonists, inverse, potent, Receptors, Histamine, histaminergic, VUF9153, VUF, 9153, Histamine, H3, Receptors, Histamine, H4, Receptors, Histamine, H3, Receptors, Tocris Bioscience
3 Citations for Clobenpropit dihydrobromide
Citations are publications that use Tocris products. Selected citations for Clobenpropit dihydrobromide include:
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
Alkan et al (2015) Histidine Decarboxylase Deficiency Prevents Autoimmune Diabetes in NOD Mice. J Immunol 2015 965056 PMID: 26090474
Hedegaard et al (2012) Molecular pharmacology of human NMDA receptors. Neurochem Int 61 601 PMID: 22197913
Do you know of a great paper that uses Clobenpropit dihydrobromide from Tocris? If so please let us know.
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