Pyrrolylquinoxalinediones carrying a piperazine residue represent highly potent and selective ligands to the homomeric kainate receptor GluR5.
Pyrrolylquinoxalinediones carrying aminoalkyl residues were evaluated for affinity to the recombinant, homomeric kainate receptors GluR5, GluR6 and GluR7. Most derivatives preferred binding to GluR5. In particular, the piperazine 6e represents a highly potent and selective antagonist to GluR5.
Department of CNS Discovery Research, Abbott GmbH & Co. KG, PO Box 210805, 67008, Ludwigshafen, Germany. wilfried.lubisch@abbott.com
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W
Lubisch
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Behl
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Henn
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Hofmann
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J
Reeb
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F
Regner
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M
Vierling
D000818:Animals; D001665:Binding Sites; D004305:Dose-Response Relationship, Drug; D018691:Excitatory Amino Acid Antagonists / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D008024:Ligands; D051379:Mice; D015394:Molecular Structure; D016202:N-Methylaspartate / Q000494:pharmacology; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism* / Q000494:pharmacology; D011810:Quinoxalines / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism* / Q000494:pharmacology; D018092:Kainic Acid Receptors / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000378:metabolism*; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy; D013329:Structure-Activity Relationship; D013379:Substrate Specificity; D018350:alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid / Q000494:pharmacology
D018691:Excitatory Amino Acid Antagonists; D008024:Ligands; D016202:N-Methylaspartate; D010879:Piperazines; D011810:Quinoxalines; D018092:Kainic Acid Receptors; D018350:alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid