Desformylflustrabromine (dFBr) is a monomethyl

tryptamine Tryptamine is an indolamine metabolite of the essential amino acid, tryptophan. The chemical structure is defined by an indole ─ a fused benzene and pyrrole ring, and a 2-aminoethyl group at the second carbon (third aromatic atom, with the f ...

derivative which was first isolated as a secondary metabolite of the marine bryozoan '' Flustra foliacea''.

Bioactivity

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. 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 Nicotinic acetylcholine receptors, or nAChRs, are receptor polypeptides that respond to the neurotransmitter acetylcholine. Nicotinic receptors also respond to drugs such as the agonist nicotine. They are found in the central and peripheral ner ...

responses by using two-electrode voltage clamp whole cell recordings. In the year 2002 it was reported that dFBr was cytotoxic on human colon cancer cell line HCT 116. 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. 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. Modulation of nicotonic 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 Neuropathic pain is pain caused by damage or disease affecting the somatosensory system. Neuropathic pain may be associated with abnormal sensations called dysesthesia or pain from normally non-painful stimuli (allodynia). It may have continuous ...

. Anti-addictive and pro-cognitive actions have also been demonstrated. Furthermore, limited experimental data suggests a potential use in treating the compulsive behaviors seen in OCD.

Bioactivity

References

Further reading