A 331440 dihydrochloride
High affinity histamine H3 receptor antagonist (Ki values are 21.7 and 22.7 nM for rat and human H3 receptors, respectively). Exhibits selectivity for human H3 over H1, H2 and H4 receptors (Ki values are 2940, 14400 and >10000 nM respectively). Shown to reduce weight in a diet-induced obesity model.
|Storage||Desiccate 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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 422.39. 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||2.37 mL||11.84 mL||23.67 mL|
|5 mM||0.47 mL||2.37 mL||4.73 mL|
|10 mM||0.24 mL||1.18 mL||2.37 mL|
|50 mM||0.05 mL||0.24 mL||0.47 mL|
References are publications that support the biological activity of the product.
Hancock et al (2004) Antiobesity effects of A-331440, a novel non-imidazole histamine H3 receptor antagonist. Eur.J.Pharmacol. 487 183 PMID: 15033391
Hancock et al (2004) In vitro optimization of structure activity relationships by analogues of A-331440 combining radioligand receptor binding assays and micronucleus assays of potential antiobesity histamine H3 receptor antagonists. Basic Clin.Pharmacol.Toxicol. 95 144 PMID: 15447739
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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.