Clobenpropit dihydrobromide

Cat. No. 0752

Clobenpropit dihydrobromide C14H17ClN4S.2HBr [145231-35-2]

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Alternative Name: VUF 9153

Chemical Name: N-(4-Chlorobenzyl)-S-[3-(4(5)-imidazolyl)propyl]isothiourea dihydrobromide

Biological Activity

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™.

Licensing Information

Sold with the permission of SCI, Amsterdam

Technical Data

M.Wt:
470.65
Formula:
C14H17ClN4S.2HBr
Solubility:
Soluble to 100 mM in water
Purity:
>99 %
Storage:
Store at RT
CAS No:
145231-35-2

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

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.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for Clobenpropit dihydrobromide include:

Alkan et al (2015) Histidine Decarboxylase Deficiency Prevents Autoimmune Diabetes in NOD Mice. J Immunol 2015 965056. PMID: 26090474.

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.

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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Keywords: Clobenpropit dihydrobromide, supplier, H4, partial, agonists, H3, antagonists, inverse, potent, Receptors, Histamine, histaminergic, VUF9153, Tocris Bioscience, Histamine H3 Receptor Antagonist products

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