2-Arylureidobenzoic Acids: Selective Noncompetitive Antagonists for the Homomeric Kainate Receptor Subtype GluR5

A series of 2-arylureidobenzoic acids (AUBAs) was prepared by a short and effective synthesis, and the pharmacological activity at glutamate receptors was evaluated in vitro and in vivo. The compounds showed noncompetitive antagonistic activity at the kainate receptor subtype GluR5. The most potent...

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Veröffentlicht in:	Journal of medicinal chemistry 2003-12, Vol.46 (26), p.5834-5843
Hauptverfasser:	Valgeirsson, Jon, Nielsen, Elsebet Ø, Peters, Dan, Varming, Thomas, Mathiesen, Claus, Kristensen, Anders S, Madsen, Ulf
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Benzoates - chemical synthesis Benzoates - pharmacology Biological and medical sciences Cell Line Excitatory Amino Acid Agonists Glutamatergic system (aspartate and other excitatory aminoacids) Humans Isoxazoles Medical sciences Mice Muscle Rigidity - chemically induced Muscle Rigidity - drug therapy Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Patch-Clamp Techniques Pharmacology. Drug treatments Propionates Quantitative Structure-Activity Relationship Radioligand Assay Receptors, Kainic Acid - antagonists & inhibitors Receptors, Kainic Acid - physiology Urea - analogs & derivatives Urea - chemical synthesis Urea - pharmacology
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