Inhibition of willardiine-induced currents through rat GluR6/KA-2 kainate receptor channels by Zinc and other divalent cations.
Heteromeric GluR6/KA-2 kainate receptor were expressed in HEK293 cells and an inhibition of willardiine-induced currents by cations was studied. Zinc was much more effective than Ca(2+), Ba(2+) and Mg(2+) at 235, 265 and 1382 fold increase in IC(50), respectively. The inhibition was not voltage-dependent. The present data showed that the binding site for the cations are different from that for willardiine and that the currents are inhibited by the cations via at least two distinct binding sites to Zn(2+) and Ca(2+). These data suggest that Zn(2+) play an important role in modulating glutamate receptors at the nervous system because of a presence of Zn(2+) and various effects of Zn(2+) on the receptors.
Fukushima
Teruyuki
T
Faculty of Engineering, Iwate University, 4-3-5 Ueda, Morioka 020-8551, Japan.
Shingai
Ryuzo
R
Ogurusu
Tarou
T
Ichinose
Mitsuyuki
M
D000409:Alanine / Q000031:analogs & derivatives* / Q000494:pharmacology*; D000818:Animals; D001464:Barium / Q000378:metabolism; D001667:Binding, Competitive; D002118:Calcium / Q000378:metabolism; D002413:Cations, Divalent / Q000378:metabolism*; D002461:Cell Line, Transformed; D004305:Dose-Response Relationship, Drug; D006801:Humans; D008274:Magnesium / Q000378:metabolism; D008564:Membrane Potentials / Q000187:drug effects*; D018408:Patch-Clamp Techniques; D011744:Pyrimidinones; D051381:Rats; D018092:Kainic Acid Receptors / Q000187:drug effects* / Q000378:metabolism; D014498:Uracil; D015032:Zinc / Q000378:metabolism; D000097806:GluK2 Kainate Receptor
D000409:Alanine; D001464:Barium; D002118:Calcium; D002413:Cations, Divalent; D008274:Magnesium; D011744:Pyrimidinones; D018092:Kainic Acid Receptors; D014498:Uracil; D015032:Zinc; D000097806:GluK2 Kainate Receptor; C002872:willardiine