Desformylflustrabromine hydrochloride

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3328/10
3328/50
Desformylflustrabromine hydrochloride | CAS No. 951322-11-5 | Nicotinic (a4b2) Receptor Modulators
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Description: Positive allosteric modulator of α4β2 nAChRs; also muscle-type nAChR inhibitor

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

Purity: ≥98%

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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

M.Wt:
357.72
Formula:
C16H21BrN2.HCl
Solubility:
Soluble to 100 mM in DMSO and to 10 mM in water with gentle warming
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
951322-11-5

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.

Background References

  1. Desformylflustrabromine (dFBr) and [3H]dFBr-labeled binding sites in a nicotinic acetylcholine receptor.
    Hamouda et al.
    Mol.Pharmacol., 2015;88:1
  2. Synthesis of desformylflustrabromine and its evaluation as an α4β2 and α7 nACh receptor modulator.
    Kim et al.
    Bioorg.Med.Chem.Lett., 2007;17:4855
  3. Potentiation of human α4β2 neuronal nicotinic receptors by a Flustra foliacea metabolite.
    Sala et al.
    Neurosci.Lett., 2005;373:44
  4. Pharmacological characterization of the allosteric modulator desformylflustrabromine and its interaction with α4β2 neuronal nicotinic acetylcholine receptor orthosteric ligands.
    Weltzin and Schulte
    J.Pharm.Exp.Ther., 2010;334:917

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