1. Department of Medicinal Chemistry, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen (Denmark), Fax: (+45)?3533‐6040 http://www.farma.ku.dk/chembiol;2. Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Science, St. Petersburg (Russia)
Abstract:
More discerning than the parent : Analogues of the polyamine toxin argiotoxin 636 (shown docked in the ion channel of an ionotropic glutamate (iGlu) receptor; N blue, O red) distinguish subtypes of iGlu receptors. Depending on which of the two internal amine groups is replaced with a methylene group, the analogue inhibits one or other of two receptor subtypes as potently as the natural compound, which itself inhibits both subtypes nonselectively.