caa a22 4500 463186907 CHVBK 20180406164856.0 cr unu---uuuuu 170326e20070801xx s 000 0 eng 10.1007/s00726-007-0520-5 doi (NATIONALLICENCE)springer-10.1007/s00726-007-0520-5 Anthraquinone polyamines: novel channel blockers of N -methyl- d -aspartate receptors [Elektronische Daten] [K. Kashiwagi, K. Williams, K. Igarashi] Summary.: Polyamines, in particular spermine, as well as some natural and synthetic polyamine derivatives have been found to be blockers of N-methyl-d-aspartate receptors. We developed novel, polyamine-based channel blockers to analyze the structure of NMDA receptors. Anthraquinone polyamines block NMDA receptors with some selectivity compared to other glutamate receptors. Results using mutant NR1 and NR2 subunits identified amino acid residues that influence blockade by anthraquinone polyamines. The head group (anthraquinone) may be positioned at the selectivity filter/narrowest constriction of the channel and the polyamine tail penetrates this constriction into the inner vestibule below the level of the selectivity filter. The results are consistent with other work showing that NR1 (Asn616) and NR2B (Asn616), but not NR2B (Asn615), make the narrowest constriction of NMDA channel, and that the M3 segments from the two subunits, which form the outer vestibule, are likely staggered relative to each other in the vertical axis of the channel. Springer-Verlag, 2007 Keywords: Polyamine derivatives - Glutamate receptor - NMDA receptor - Channel blocker nationallicence AMPA : α-aminio-3-hydroxy-5-methyl-4-isoxazolepropionic acid nationallicence AQP : anthraquinone polyamine nationallicence AQ33 : N 1-(anthraquinone-2-carbonyl)norspermidine nationallicence AQ33b : 4-(anthraquinone-2-carbonyl)-4-azaheptane-1,7-diamine nationallicence AQ34 : N 1-(anthraquinone-2-carbonyl)spermidine nationallicence AQ343 : N 1-(anthraquinone-2-carbonyl)spermine nationallicence AQ444 : N 1-(anthraquinone-2-carbonyl)homospermine nationallicence MK801 : dizocilpine maleate nationallicence NMDA : N-methyl-d-aspartate nationallicence TB34 : N 1,N 4,N 8-tribenzylspermidine nationallicence Kashiwagi K. Faculty of Pharmacy, Chiba Institute of Science, Choshi, Japan aut Williams K. Department of Physiology and Pharmacology, State University of New York Downstate Medical Center, Brooklyn, New York, USA aut Igarashi K. Graduate School of Pharmaceutical Sciences, Chiba University, Chiba, Japan aut Amino Acids Springer-Verlag 33/2(2007-08-01), 299-304 0939-4451 33:2<299 2007 33 726 https://doi.org/10.1007/s00726-007-0520-5 text/html Onlinezugriff via DOI 1 review-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/s00726-007-0520-5 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Kashiwagi K. Faculty of Pharmacy, Chiba Institute of Science, Choshi, Japan aut NATIONALLICENCE 700 1- Williams K. Department of Physiology and Pharmacology, State University of New York Downstate Medical Center, Brooklyn, New York, USA aut NATIONALLICENCE 700 1- Igarashi K. Graduate School of Pharmaceutical Sciences, Chiba University, Chiba, Japan aut NATIONALLICENCE 773 0- Amino Acids Springer-Verlag 33/2(2007-08-01), 299-304 0939-4451 33:2<299 2007 33 726 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer