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 α4β2nicotinic 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 deconstructed analogs of dFBr are reported to have a potentiating effect on the α4β2 receptors.[6]
References
^Peters, Lars; Wright, Anthony D.; Kehraus, Stefan; Gündisch, Daniela; Tilotta, M. C.; König, Gabriele M. (October 2004). "Prenylated indole alkaloids from Flustra foliacea with subtype specific binding on NAChRs". Planta Med. 70 (10): 883–6. doi:10.1055/s-2004-832610. PMID15490312.
^Sala, Francisco; Mulet, José; Reddy, Krishna P.; Bernal, José Antonio; Wikman, Philip; Valor, Luis Miguel; Peters, Lars; König, Gabriele M.; Criado, Manuel (January 2005). "Potentiation of human alpha4beta2 neuronal nicotinic receptors by a Flustra foliacea metabolite". Neurosci. Lett. 373 (2): 144–9. doi:10.1016/j.neulet.2004.10.002. PMID15567570.
^Lysek, N; Rachor, E; Lindel, T (2002). "Isolation and structure elucidation of deformylflustrabromine from the North Sea bryozoan Flustra foliacea". Z. Naturforsch. C. 57 (11–12): 1056–61. PMID12562094.
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