CAS NO: | 314-13-6 |
包装: | 1g |
规格: | 98% |
市场价: | 629元 |
分子量: | 960.82 |
Background:
IC50: 220 and 150 nM for GluRl and GIuR6, respectively.
Evans Blue tetrasodium salt is a potent inhibitor of AMPA and kainate receptor-mediated currents (GluRl and GIuR6).
Pharmacologically, the glutamate transporter is specific for glutamate and the closely related analogue L-aspartate does not block the uptake, whereas agents like L-homocysteate and La- aminoadipate block the vesicular L-glutamate uptake poorly.
In vitro: Evans blue inhibits the kainate-mediated responses of the non-NMDA receptor subunits (GIuRl, G1uR1,2, G1uRl,3, and G1uR2,3) expressed in Xenopus oocytes without the response of GluR3 and G1uR6 at low concentrations (IC50= 355 nM for the subunit combination GluR1,2). This pocess was partially reversible without competing with kainate for the agonist binding site [1]. In whole-cell patch clamp recordings of transfected human embryonic kidney 293 cells, Evans blue is a potent inhibitor of glutamate-evoked currents mediated by the kainate-type receptor GIuR6 as long as the AMPA-type receptor GluRl. Interestingly, pretreating with the lectin concanavalin cells recorded relatively little EB inhibition of GIuR6 currents, eliminating kainate receptor desensitization. In addition to decreasing GluR6-mediated peak current amplitude, EB significantly changed receptor desensitization by slowing the rate of onset by