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Positive allosteric modulator of nicotinic α4β2 receptors; selectively increases the ionic current through α4β2 in the presence of ACh. Displays 14.7-fold selectivity for α4β2 over homomeric (α7) receptors. Moderately cytotoxic in HCT-116 cells. Also inhibits human muscle (αβεδ) and Torpedo (αβγδ) nAChRs (IC50 values are 1.0 and 0.1 μM, respectively) by binding in the ion channel.
|Storage||Store at +4°C|
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|
|water||3.58||10 with gentle warming|
Preparing Stock Solutions
The following data is based on the product molecular weight 357.72. 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||2.8 mL||13.98 mL||27.95 mL|
|5 mM||0.56 mL||2.8 mL||5.59 mL|
|10 mM||0.28 mL||1.4 mL||2.8 mL|
|50 mM||0.06 mL||0.28 mL||0.56 mL|
References are publications that support the biological activity of the product.
Kim et al (2007) Synthesis of desformylflustrabromine and its evaluation as an α4β2 and α7 nACh receptor modulator. Bioorg.Med.Chem.Lett. 17 4855 PMID: 17604168
Sala et al (2005) Potentiation of human α4β2 neuronal nicotinic receptors by a Flustra foliacea metabolite. Neurosci.Lett. 373 44
Weltzin and Schulte (2010) Pharmacological characterization of the allosteric modulator desformylflustrabromine and its interaction with α4β2 neuronal nicotinic acetylcholine receptor orthosteric ligands. J.Pharm.Exp.Ther. 334 917
Hamouda et al (2015) Desformylflustrabromine (dFBr) and [3H]dFBr-labeled binding sites in a nicotinic acetylcholine receptor. Mol.Pharmacol. 88 1 PMID: 25870334
If you know of a relevant reference for Desformylflustrabromine hydrochloride, please let us know.
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Keywords: Desformylflustrabromine hydrochloride, Desformylflustrabromine hydrochloride supplier, dFBr, a4b2, nicotinic, acetylcholine, receptor, receptors, nAChR, positive, allosteric, modulators, PAM, Nicotinic, (a4b2), Receptors, (Other, Subtypes), 3328, Tocris Bioscience
Citations for Desformylflustrabromine hydrochloride
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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.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.