Cat. No. 3328
Chemical Name: 6-Bromo-2-(1,1-dimethyl-2-propenyl)
Biological ActivityPositive 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.
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 / Safety Data Sheet
Hamouda et al (2015) Desformylflustrabromine (dFBr) and [3H]dFBr-labeled binding sites in a nicotinic acetylcholine receptor. Mol.Pharmacol. 88 1. PMID: 25870334.
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.
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.
If you know of a relevant reference for this product please let us know.
Citations are publications that use Tocris products.
Do you know of a great paper that uses Desformylflustrabromine hydrochloride from Tocris? If so please let us know.
View Related Products by Product Action
Keywords: Desformylflustrabromine hydrochloride, supplier, dFBr, a4b2, nicotinic, acetylcholine, receptor, receptors, nAChR, positive, allosteric, modulators, Tocris Bioscience, Nicotinic (α4β2) Receptor Modulator products
Find multiple products by catalog number
Follow @Tocris on Twitter
Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.