[Thieno[2,3-d]pyrimidines as antagonists of the glutamate receptors].
Although the function of the kainate receptors in the brain is still not clear, they are increasingly defined as targets in the development of new classes of anti-epileptics. The thienopyrimidines described in this report were tested for their antagonistic effect at the kainate receptor subtypes GluR5 and GluR6. The highest effectiveness was obtained by a 4-ethoxy-thieno[2,3-d]pyrimidin with an IC50 = 68 microM at the GluR6 receptor.
Briel
D
D
Pharmazeutische Chemie, Institut für Pharmazie, Fakultät für Biowissenschaften, Pharmazie und Psychologie, Universität Leipzig, Leipzig, Germany. briel@rz.uni-leipzig.de
Rybak
A
A
Kronbach
C
C
Unverferth
K
K
D001923:Brain Chemistry / Q000187:drug effects; D002478:Cells, Cultured; D018691:Excitatory Amino Acid Antagonists / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D011743:Pyrimidines / Q000494:pharmacology*; D017470:Receptors, Glutamate / Q000187:drug effects*; D018092:Kainic Acid Receptors / Q000037:antagonists & inhibitors / Q000378:metabolism; D000097806:GluK2 Kainate Receptor
D018691:Excitatory Amino Acid Antagonists; D007202:Indicators and Reagents; D011743:Pyrimidines; D017470:Receptors, Glutamate; D018092:Kainic Acid Receptors; D000097806:GluK2 Kainate Receptor