培养细胞对（-）-去甲肾上腺素的摄取与代谢
The accumulation and metabolism of (-)-noradrenaline by cells in culture.
作者信息
Powis G
出版信息
Br J Pharmacol. 1973 Mar;47(3):568-75. doi: 10.1111/j.1476-5381.1973.tb08187.x.
Abstract
- Cultured bovine embryonic tracheal cells, EbTr (NBL-4) possess a process for the intracellular accumulation of (-)-noradrenaline with the characteristics generally ascribed to extraneuronal uptake by cardiac and smooth muscle cells in the body. It has a K(m) of 2.6 x 10(-4)M.2. The accumulation process is inhibited competitively by normetanephrine, but only at relatively high concentrations, IC50=2.1 x 10(-4)M. Inhibition also occurs with 17-beta-oestradiol, IC50=1.3 x 10(-5)M.3. The noradrenaline metabolites, 3,4-dihydroxy-mandelic acid and 3,4-dihydroxy-phenylglycol potentiate accumulation and reduce intracellular levels of normetanephrine in a similar manner to known inhibitors of catechol-O-methyl transferase.4. It is suggested that intracellular, rather than extracellular, normetanephrine may exert feedback inhibition upon noradrenaline accumulation by combining with the transport process at the inner surface of the cell membrane.
摘要
培养的牛胚胎气管细胞EbTr（NBL-4）具有将（-）-去甲肾上腺素进行细胞内积累的过程，其特征与体内心脏和平滑肌细胞的非神经元摄取过程通常所具有的特征相同。其米氏常数（K(m)）为2.6×10⁻⁴M。
去甲肾上腺素代谢产物间甲去甲肾上腺素可竞争性抑制该积累过程，但仅在相对较高浓度时才会发生，半数抑制浓度（IC50）为2.1×10⁻⁴M。17-β-雌二醇也会产生抑制作用，IC50为1.3×10⁻⁵M。
去甲肾上腺素代谢产物3,4-二羟基扁桃酸和3,4-二羟基苯乙二醇以与已知儿茶酚-O-甲基转移酶抑制剂类似的方式增强积累并降低细胞内间甲去甲肾上腺素水平。
有人提出，细胞内而非细胞外的间甲去甲肾上腺素可能通过与细胞膜内表面的转运过程结合，对去甲肾上腺素的积累产生反馈抑制作用。
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