Desformylflustrabromine hydrochloride

Cat. No. 3328

Desformylflustrabromine hydrochloride C16H21BrN2.HCl [951322-11-5]

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Chemical Name: 6-Bromo-2-(1,1-dimethyl-2-propenyl)-N-1H-indole-3-ethanamine hydrochloride

Biological Activity

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.

Technical Data

Soluble to 100 mM in DMSO and to 10 mM in water with gentle warming
>98 %
Store at +4°C

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 Datasheet

References are publications that support the products' biological activity.

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.

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Keywords: Desformylflustrabromine hydrochloride, supplier, dFBr, a4b2, nicotinic, acetylcholine, receptor, receptors, nAChR, positive, allosteric, modulators, Tocris Bioscience, Nicotinic (α4β2) Receptor Modulator products

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