Torres M, Fideu M D, Miras-Portugal M T
Departamento Bioquímica, Facultad de Veterinaria, Universidad Complutense de Madrid, Spain.
Neurosci Lett. 1990 May 4;112(2-3):343-7. doi: 10.1016/0304-3940(90)90228-2.
Nitrobenzylthioinosine is an effective inhibitor of adenosine transport in chromaffin cells. When adenosine transport was measured at a 0.15 microM adenosine concentration, in the presence of variable concentrations of nitrobenzylthioinosine, ranging from 10(-14) to 10(-6) M, a half-maximal inhibitory concentration value (IC50) of 1 +/- 0.3 nM was deduced. This compound has the capacity to inhibit the total adenosine transport at 10(-7) M concentration. Nitrobenzylthioinosine acts in a non-competitive manner in blocking adenosine transport, as deduced from a Dixon plot, with a constant inhibition value (K1) of 0.01 +/- 0.003 nM. The results suggest that all nucleoside transporters present in bovine chromaffin cells are sensitive to the nitrobenzylthioinosine inhibition.
硝基苄硫基肌苷是嗜铬细胞中腺苷转运的有效抑制剂。当在0.15微摩尔腺苷浓度下,在10⁻¹⁴至10⁻⁶摩尔可变浓度的硝基苄硫基肌苷存在下测量腺苷转运时,推导出半数最大抑制浓度值(IC50)为1±0.3纳摩尔。该化合物在10⁻⁷摩尔浓度下具有抑制总腺苷转运的能力。从狄克逊图推导可知,硝基苄硫基肌苷以非竞争性方式阻断腺苷转运,恒定抑制值(K1)为0.01±0.003纳摩尔。结果表明,牛嗜铬细胞中存在的所有核苷转运体对硝基苄硫基肌苷抑制敏感。