Synthesis of desformylflustrabromine and its evaluation as an alpha4beta2 and alpha7 nACh receptor modulator.

Autor: Kim JS; Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298, USA., Padnya A, Weltzin M, Edmonds BW, Schulte MK, Glennon RA
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Sep 01; Vol. 17 (17), pp. 4855-60. Date of Electronic Publication: 2007 Jun 14.
DOI: 10.1016/j.bmcl.2007.06.047
Abstrakt: Desformylflustrabromine (dFBr; 1) and desformylflustrabromine-B (dFBr-B; 2) have been previously isolated from natural sources, and the former has been demonstrated to be a novel and selective positive allosteric modulator of alpha4beta2 nicotinic acetylcholine (nACh) receptors. The present study describes the synthesis of water-soluble salts of 1 and 2, and confirms and further investigates the actions of 1 and 2 using two-electrode voltage clamp recordings.
Databáze: MEDLINE