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Design, total synthesis, and biological evaluation of neodysiherbaine A derivative as potential probes
Authors:Sasaki Makoto  Tsubone Koichi  Shoji Muneo  Oikawa Masato  Shimamoto Keiko  Sakai Ryuichi
Affiliation:Laboratory of Biostructural Chemistry, Graduate School of Life Sciences, Tohoku University, Sendai 981-8555, Japan. masasaki@bios.tohoku.ac.jp
Abstract:To enable studies to elucidate the detailed biological function of dysiherbaine and neodysiherbaine A, potent and subunit-selective agonists for ionotropic glutamate receptors, the derivative with a hydroxymethyl substituent at the C10 position has been developed. Preliminary biological evaluation of the analogue showed that a C10 hydroxymethyl substituent produced significant alterations in binding affinities for the ionotropic glutamate receptor subtypes.
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