KN-62, a calcium calmodulin-dependent protein kinase II inhibitor, inhibits high potassium-stimulated prolactin secretion and intracellular calcium increases in anterior pituitary cells
KN-62, a calcium calmodulin-dependent protein kinase II inhibitor, inhibits high potassium-stimulated prolactin secretion and intracellular calcium increases in anterior pituitary cells
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DOI：
10.1016/0167-4889(95)00170-0
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发表时间：
1996-02-29
影响因子：
5.1
通讯作者：
Dannies, PS
中科院分区：
文献类型：
--
作者：
Cui, ZJ;Hidaka, H;Dannies, PS
在分离的大鼠垂体前叶细胞上，钙/钙调素依赖的蛋白激酶II的异喹啉磺胺抑制剂KN-62(10 MM)几乎完全抑制KCl50 mM刺激的催乳素分泌，IC50为95 nM。KN-62对TRH诱导的催乳素分泌的抑制作用较弱。KN-04是一种活性降低100倍以上的化合物，它抑制纯化的钙/钙调素依赖的蛋白激酶II：也抑制KCl2刺激的催乳素的高分泌，IC50为500 nM。KN-62和KN-04(10mU M)均能抑制高钾刺激的细胞内钙离子浓度的升高。我们得出结论，KN-62和KN-04直接或间接地抑制垂体前叶细胞电压依赖性钙通道的激活。
In isolated rat anterior pituitary cells, KN-62 (10 mu M), an isoquinoline sulfonamide inhibitor of calcium/calmodulin-dependent protein kinase II, inhibited high KCl(50 mM)-stimulated prolactin secretion almost completely, with an IC50 of 95 nM. KN-62 inhibited TRH-induced prolactin secretion less effectively. KN-04, a compound that is over 100-fold less active in inhibiting purified calcium/calmodulin-dependent protein kinase II: also inhibited high KCl-stimulated prolactin secretion with an IC50 of 500 nM. KN-62 and KN-04 (10 mu M) both inhibited high KCl-stimulated increases in intracellular Ca2+ concentrations. We conclude that KN-62 and KN-04 inhibit activation of voltage-dependent calcium channels in anterior pituitary cells either directly or indirectly.