Endoxifen is a new potent inhibitor of PKC: A potential therapeutic agent for bipolar disorder
Endoxifen is a new potent inhibitor of PKC: A potential therapeutic agent for bipolar disorder
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DOI：
10.1016/j.bmcl.2010.02.024
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发表时间：
2010-04-15
影响因子：
2.7
通讯作者：
Ahmad, Imran
中科院分区：
文献类型：
--
作者：
Ali, Shoukath M.;Ahmad, Ateeq;Ahmad, Imran
蛋白激酶C(PKC)在突触前和突触后的神经传递调节中起着重要作用。PKC的过度激活会导致与双相情感障碍相关的症状。他莫昔芬是一种广泛使用的乳腺癌药物，已知能抑制PKC并显示出抗躁狂特性。本文报道了他莫昔芬活性代谢物Enoxifen的合成，并与他莫昔芬的PKC抑制活性进行了比较。与他莫昔芬相比，艾多昔芬的效力高出四倍。(C)2010爱思唯尔有限公司。保留所有权利。
Protein kinase C (PKC) plays a major role in regulation of both pre and postsynaptic neurotransmission. Excessive activation of PKC results in symptoms related to bipolar disorder. Tamoxifen, a widely used breast cancer drug is known to inhibit PKC and demonstrate antimanic properties in human. We describe herein the synthesis of endoxifen, a tamoxifen active metabolite and compared its PKC inhibitory activity with that of tamoxifen. Endoxifen exhibited fourfold higher potency compared to tamoxifen. (C) 2010 Elsevier Ltd. All rights reserved.