Bender A S, Hertz L
Department of Pharmacology, University of Saskatchewan, Saskatoon, Canada.
Neurochem Res. 1986 Nov;11(11):1507-24. doi: 10.1007/BF00965770.
Uptake of extracellular adenosine was studied in primary cultures of astrocytes or neurons. Both cell types showed a high affinity uptake. The Km values were not significantly different (6.5 +/- 3.75 microM in astrocytes and 6.1 +/- 1.86 microM in neurons), but the intensity of the uptake was higher in astrocytes than in neurons (Vmax values of 0.16 +/- 0.030 and 0.105 +/- 0.010 nmol x min-1 x mg-1 protein, respectively). The temperature sensitivity was similar in the two cell types. Adenosine uptake inhibitors and benzodiazepines inhibited the adenosine uptake systems in both astrocytes and neurons with IC50 values in the high nanomolar or the micromolar range and the rank order of potency was similar in the two cell types. In both cell types the (-) isomers of two sets of benzodiazepine stereoisomers were more potent than the (+) isomers. Dixon analysis showed that dipyridamole, papaverine, hexobendine and chlordiazepoxide inhibited the adenosine uptake competitively and clonazepam noncompetitively in both cell types.
在星形胶质细胞或神经元的原代培养物中研究了细胞外腺苷的摄取。两种细胞类型均表现出高亲和力摄取。Km值无显著差异(星形胶质细胞中为6.5±3.75微摩尔,神经元中为6.1±1.86微摩尔),但星形胶质细胞中的摄取强度高于神经元(Vmax值分别为0.16±0.030和0.105±0.010纳摩尔·分钟-1·毫克-1蛋白质)。两种细胞类型的温度敏感性相似。腺苷摄取抑制剂和苯二氮䓬类药物抑制星形胶质细胞和神经元中的腺苷摄取系统,IC50值在高纳摩尔或微摩尔范围内,两种细胞类型的效价顺序相似。在两种细胞类型中,两组苯二氮䓬类立体异构体的(-)异构体比(+)异构体更有效。Dixon分析表明,双嘧达莫、罂粟碱、己酮可可碱和氯氮䓬在两种细胞类型中均竞争性抑制腺苷摄取,而氯硝西泮则非竞争性抑制。