Desformylflustrabromine

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Desformylflustrabromine is an active metabolite of marine bryozoan Flustra foliacea.[1] Desformylflustrabromine has been identified a novel positive allosteric modulator of neuronal nicotinic acetylcholine receptor with sub-type specificity for hetromeric receptor with no effect on homomeric sub-type.[2] A recent study has been published which describes the synthesis of water-soluble salts of Desformylflustrabromine and its action has been confirmed as selective potentiator of alpha4 beta2 receptor responses by using two-electrode voltage clamp whole cell recordings.[3]

References

  1. Peters, L.; Wright, A. D.; Kehraus, S.; Gündisch, D.; Tilotta, M. C.; König, G. M. Planta Med. 2004, 70, 883.
  2. Sala, F.; Mulet, J.; Reddy, K. P.; Bernal, J. A.; Wikman, P.; Valor, L. M.; Peters, L.; Konig, G. M.; Criado, M.; Sala, S. Neurosci. Lett. 2005, 373, 144
  3. Jin-Sung Kim, Anshul Pandya, Maegan Weltzin, Brian W. Edmonds, Marvin K. Schulte, and Richard A. Glennon. Synthesis of desformylflustrabromine and its evaluation as an alpha4beta2 and alpha7 nACh receptor modulator. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4855-60. Epub 2007 Jun.

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