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原代星形胶质细胞培养物对[3H]去甲肾上腺素的高亲和力摄取及其受三环类抗抑郁药的抑制作用。

High-affinity uptake of [3H]norepinephrine by primary astrocyte cultures and its inhibition by tricyclic antidepressants.

作者信息

Kimelberg H K, Pelton E W

出版信息

J Neurochem. 1983 May;40(5):1265-70. doi: 10.1111/j.1471-4159.1983.tb13565.x.

Abstract

Primary astrocyte cultures from neonatal rat brains show uptake of [3H]norepinephrine ([3H]NE). This uptake has a high-affinity component with an apparent Km of approximately 3 X 10(-7) M. At 10(-7) M [3H]NE both the initial rate of uptake and steady-state content of [3H]NE is inhibited by up to 95% by omission of external Na+. The Na+-dependent component of this uptake is totally inhibited by the tricyclic antidepressants desipramine (DMI) and amitryptyline with IC50 values of 2 X 10(-9) and 4 X 10(-8) M, respectively. Inhibition of [3H]NE uptake by DMI shows competitive kinetics. These characteristics are essentially identical to those found for high-affinity uptake of NE in total membrane or synaptosome fractions from rodent brains and suggests that such uptake in neural tissue is not exclusively neuronal.

摘要

新生大鼠脑的原代星形胶质细胞培养物显示出对[3H]去甲肾上腺素([3H]NE)的摄取。这种摄取具有高亲和力成分,其表观Km约为3×10(-7)M。在10(-7)M [3H]NE时,外部Na +的缺失会使[3H]NE的初始摄取速率和稳态含量受到高达95%的抑制。这种摄取的Na +依赖性成分被三环类抗抑郁药地昔帕明(DMI)和阿米替林完全抑制,IC50值分别为2×10(-9)和4×10(-8)M。DMI对[3H]NE摄取的抑制表现出竞争性动力学。这些特征与在啮齿动物脑的总膜或突触体部分中发现的NE高亲和力摄取的特征基本相同,这表明神经组织中的这种摄取并非仅由神经元完成。

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