Positive allosteric modulator of nicotinic α
2 receptors; selectively increases the ionic current through α
2 in the presence of ACh. Displays 14.7-fold selectivity for α
2 over homomeric (α
7) receptors. Moderately cytotoxic in HCT-116 cells. Also inhibits human muscle (αβεδ
) and Torpedo
) nAChRs (IC50
values are 1.0 and 0.1 μ
M, respectively) by binding in the ion channel.
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All Tocris products are intended for laboratory research use only.
Synthesis of desformylflustrabromine and its evaluation as an α4β2 and α7 nACh receptor modulator.
Kim et al.
Potentiation of human α4β2 neuronal nicotinic receptors by a Flustra foliacea metabolite.
Sala et al.
Desformylflustrabromine (dFBr) and [3H]dFBr-labeled binding sites in a nicotinic acetylcholine receptor.
Ayman et al.