[Thieno[2,3-d]pyrimidines as antagonists of the glutamate receptors]

D Briel; A Rybak; C Kronbach; K Unverferth

[Thieno[2,3-d]pyrimidines as antagonists of the glutamate receptors]

Pharmazie. 2008 Nov;63(11):823-6.

[Article in German]

Authors

D Briel¹, A Rybak, C Kronbach, K Unverferth

Affiliation

¹ Pharmazeutische Chemie, Institut für Pharmazie, Fakultät für Biowissenschaften, Pharmazie und Psychologie, Universität Leipzig, Leipzig, Germany. [email protected]

PMID: 19069244

Abstract

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.

Publication types

English Abstract

MeSH terms

Brain Chemistry / drug effects
Cells, Cultured
Excitatory Amino Acid Antagonists / chemical synthesis
Excitatory Amino Acid Antagonists / pharmacology*
GluK2 Kainate Receptor
Humans
Indicators and Reagents
Magnetic Resonance Spectroscopy
Pyrimidines / pharmacology*
Receptors, Glutamate / drug effects*
Receptors, Kainic Acid / antagonists & inhibitors
Receptors, Kainic Acid / metabolism

Substances

Excitatory Amino Acid Antagonists
Gluk1 kainate receptor
Indicators and Reagents
Pyrimidines
Receptors, Glutamate
Receptors, Kainic Acid