PT  - JOURNAL ARTICLE
AU  - R Bleakman
AU  - D D Schoepp
AU  - B Ballyk
AU  - H Bufton
AU  - E F Sharpe
AU  - K Thomas
AU  - P L Ornstein
AU  - R K Kamboj
TI  - Pharmacological discrimination of GluR5 and GluR6 kainate receptor subtypes by (3S,4aR,6R,8aR)-6-[2-(1(2)H-tetrazole-5-yl)ethyl]decahyd roisdoquinoline-3 carboxylic-acid.
DP  - 1996 Apr 01
TA  - Molecular Pharmacology
PG  - 581--585
VI  - 49
IP  - 4
4099  - http://molpharm.aspetjournals.org/content/49/4/581.short
4100  - http://molpharm.aspetjournals.org/content/49/4/581.full
SO  - Mol Pharmacol1996 Apr 01; 49
AB  - The pharmacological tools available for the discrimination of kainate receptor subtypes are limited. We examined the effects of (3S,4aR,6R,8aR)-6-[2-(1(2)H-tetrazole-5-yl)ethyl]decahydr oisoquinoline-3-carboxylic acid (LY293558) and 2,3-dihydroxy-6-nitro-7-sulfamoyl-benzo[f]quinoxaline (NBQX) on inward currents associated with activation of non-N-methyl-D-asparate (NMDA) receptors in acutely isolated rat cerebellar Purkinje neurons, rat dorsal root ganglion neurons, and human embryonic kidney 293 cells transfected with human glutamate receptors (GluR) 5 and 6. LY293558 and NBQX inhibited kainate-induced currents in cerebellar Purkinje cells, DRG neurons, and human GluR5-transfected cells. In contrast, human embryonic kidney 293 cells expressing GluR6 receptors, although blocked by NBQX, were unaffected by LY293558 at concentrations of < / = 100 microM. The selective antagonism by LY293558 of GluR5 receptors should allow the determination of the functional role of GluR5 and GluR6 in more complex systems.