培养的嗜铬细胞对[3H] - 尼古丁和[3H] - 去甲肾上腺素的摄取。
Uptake of [3H]-nicotine and [3H]-noradrenaline by cultured chromaffin cells.
作者信息
Ceña V, García A G, Montiel C, Sánchez-García P
出版信息
Br J Pharmacol. 1984 Jan;81(1):119-23. doi: 10.1111/j.1476-5381.1984.tb10751.x.
Abstract
Three day-old cultured bovine adrenal chromaffin cells incubated at room temperature with Krebs-HEPES solution containing different concentrations of [3H]-nicotine, took up and retained increasing amounts of the drug by a mechanism that did not saturate. Concentrations of cold nicotine as high as 100 microM did not alter the amount of [3H]-nicotine retained by cells. Imipramine, cocaine, tetracaine or mecamylamine, at concentrations (10 microM) that blocked the catecholamine secretory effects of nicotine completely, did not modify the uptake of [3H]-nicotine. Both imipramine and cocaine drastically inhibited [3H]-noradrenaline uptake by cells in a concentration-dependent manner (IC50S of 0.08 and 1 microM, respectively). These data indicate that the secretory effects of nicotine are not coupled to its previous uptake into cells, and are evidence in favour of a site of action for nicotine located in or at the surface of the chromaffin cell membrane.
摘要
将三天龄的培养牛肾上腺嗜铬细胞在室温下与含有不同浓度[3H] - 尼古丁的Krebs - HEPES溶液一起孵育，细胞通过一种不饱和机制摄取并保留了越来越多的该药物。高达100 microM的冷尼古丁浓度并未改变细胞保留的[3H] - 尼古丁量。浓度为10 microM的丙咪嗪、可卡因、丁卡因或美加明完全阻断了尼古丁的儿茶酚胺分泌作用，但并未改变[3H] - 尼古丁的摄取。丙咪嗪和可卡因均以浓度依赖性方式强烈抑制细胞对[3H] - 去甲肾上腺素的摄取（IC50分别为0.08和1 microM）。这些数据表明，尼古丁的分泌作用与其先前进入细胞的过程无关，这支持了尼古丁的作用位点位于嗜铬细胞膜内或表面的观点。
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