The Na+-Ca2+ exchange inhibitor KB-R7943 inhibits high K+-induced increases in intracellular Ca2+ concentration and [3H]noradrenaline release in the human neuroblastoma SH-SY5Y.
The effects of the Na+-Ca2+ exchange inhibitor 2-[2-[4-(4-nitrobenzyloxy)phenyl]ethyl]isothiourea methanesulfonate (KB-R7943) on depolarization-induced Ca2+ signal and [3H]noradrenaline release were examined in SH-SY5Y cells. KB-R7943 at 10 microM significantly inhibited high K+-induced increase in intracellular Ca2+ concentration. KB-R7943 also inhibited high K+-evoked release of [3H]noradrenaline from the cells. These findings suggest that the Na+-Ca2+ exchanger in the reverse mode is involved at least partly in depolarization-induced transmitter release.
Nakamura
H
H
Laboratory of Molecular Neuropharmacology, Graduate School of Pharmaceutical Sciences, Osaka University, Suita, Japan.
Kawasaki
Y
Y
Arakawa
N
N
Saeki
M
M
Maeda
S
S
Koyama
Y
Y
Baba
A
A
Matsuda
T
T
D002118:Calcium / Q000378:metabolism*; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D007424:Intracellular Fluid / Q000201:enzymology / Q000378:metabolism; D009447:Neuroblastoma; D009638:Norepinephrine / Q000378:metabolism*; D011188:Potassium / Q000494:pharmacology*; D019831:Sodium-Calcium Exchanger / Q000037:antagonists & inhibitors*; D013890:Thiourea / Q000031:analogs & derivatives* / Q000494:pharmacology; D014316:Tritium; D014407:Tumor Cells, Cultured
C101670:2-(2-(4-(4-nitrobenzyloxy)phenyl)ethyl)isothiourea methanesulfonate; D004791:Enzyme Inhibitors; D019831:Sodium-Calcium Exchanger; D014316:Tritium; D013890:Thiourea; D011188:Potassium; D002118:Calcium; D009638:Norepinephrine