Desformylflustrabromine (dFBr) is a monomethyltryptamine derivative which was first isolated as a secondary metabolite of the marine bryozoan Flustra foliacea.[1]
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Formula | C16H21BrN2 |
Molar mass | 321.262 g·mol−1 |
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dFBr has been identified as a novel positive allosteric modulator of neuronal nicotinic acetylcholine 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 of α4β2 nicotinic 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 line HCT 116.[4]
Desformylflustrabromine has also been found to be a positive allosteric modulator for the α2β2 subtype of neuronal nicotinic acetylcholine 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 of Alzheimer'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 produce analgesic and anti-allodynic effects in animal models, which could potentially make it of interest for the treatment of neuropathic 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 the compulsive behaviors seen in OCD.[12]