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| Formula | C16H21BrN2 |
| Molar mass | 321.262 g·mol−1 |
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Desformylflustrabromine (dFBr) is anNMT derivative indole alkaloid which was first isolated from the marinebryozoanFlustra foliacea.[1]
dFBr has been identified as a novel positiveallosteric modulator of neuronal nicotinicacetylcholine receptor with sub-type specificity for heteromeric receptor with no effect on homomeric sub-type.[2] A recent study has been published which describes the synthesis of water-soluble salts of dFBr and its action has been confirmed as selective potentiator ofα4β2nicotinic acetylcholine receptor responses by using two-electrode voltage clamp whole cell recordings.[3] In the year 2002 it was reported that dFBr was cytotoxic on human colon cancer cell lineHCT 116.[4]
Desformylflustrabromine has also been found to be a positive allosteric modulator for the α2β2 subtype of neuronal nicotinicacetylcholine receptor. Additionally it relieves the inhibition of both α2β2 and α4β2 nicotinic acetylcholine receptors by β-Amyloid (1–42) Peptide.[5] Thus desformylflustrabromine can potentially be used in the treatment ofAlzheimer's disease. Many of the analogues and derivatives of dFBr are reported to have a potentiating effect on the α4β2 receptors.[6][7]
Modulation of nicotinic acetylcholine receptor function by desformylflustrabromine has also been found to produceanalgesic and anti-allodynic effects in animal models, which could potentially make it of interest for the treatment ofneuropathic pain.[8][9] Anti-addictive and pro-cognitive actions have also been demonstrated.[10][11] Furthermore, limited experimental data suggests a potential use in treating thecompulsive behaviors seen inOCD.[12]
