The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 
 
 

Identification of a subunit-specific antagonist of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate/kainate receptor channels.

Excitatory synaptic transmission in the mammalian central nervous system is mediated predominantly by glutamate receptor (GluR) channels of the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate/kainate (AMPA/KA) receptor type. A major improvement in our understanding of glutamatergic synaptic transmission has been achieved after the identification of quinoxalinediones (e.g., 6-cyano-7-nitroquinoxaline-2,3-dione) as specific antagonists of AMPA/KA receptors. In addition to their effects on neurons, quinoxalinediones were also shown to block glutamate-induced responses mediated by recombinant AMPA/KA receptor channels expressed in heterologous systems, irrespective of their particular subunit composition. Here we report the identification of an AMPA/KA receptor antagonist that selectively blocks a subset of AMPA/KA receptors. We found that Evans blue, a biphenyl derivative of naphthalene disulfonic acid, blocks at low concentrations (IC50 = 355 nM for the subunit combination GluR1,2) KA-mediated responses of the subunits GluR1, GluR1,2, GluR1,3, and GluR2,3 expressed in Xenopus oocytes but not responses of GluR3 or GluR6. The blocking action of Evans blue was partially reversible and did not compete with KA for the agonist binding site. These findings suggest not only that Evans blue is a potent tool for elucidating the functional role of specific AMPA/KA receptor subtypes for excitatory synaptic transmission but also that it may also represent a powerful starting point for clinically useful drugs that are able to reduce the excitatory drive in specific neuronal populations of the central nervous system.[1]

References

  1. Identification of a subunit-specific antagonist of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate/kainate receptor channels. Keller, B.U., Blaschke, M., Rivosecchi, R., Hollmann, M., Heinemann, S.F., Konnerth, A. Proc. Natl. Acad. Sci. U.S.A. (1993) [Pubmed]
 
WikiGenes - Universities