Torres M, Molina P, Miras-Portugal M T
FEBS Lett. 1986 May 26;201(1):124-8. doi: 10.1016/0014-5793(86)80583-x.
Chromaffin cells from bovine adrenal medulla are a useful model to approach adenosine transport and metabolism in neural cells. Dipyridamol has been shown to be an adenosine transport inhibitor with high affinity. To quantify the adenosine transporters a labelled dipyridamol analogue, [14C]dipyridamol acetate, was synthesized. This compound had a Ki = 5.3 +/- 0.43 nM according to the Dixon method, and 4.58 +/- 0.46 nM when the receptor number molarity was taken into account showing, like dipyridamol, a non-competitive mechanism. The high-affinity receptors present in chromaffin cells showed a Kd = 6.8 +/- 0.8 nM and the receptor number was 630 000 +/- 40 000 per cell.
来自牛肾上腺髓质的嗜铬细胞是研究神经细胞中腺苷转运和代谢的有用模型。双嘧达莫已被证明是一种具有高亲和力的腺苷转运抑制剂。为了定量腺苷转运体,合成了一种标记的双嘧达莫类似物[14C]双嘧达莫乙酸盐。根据迪克森方法,该化合物的Ki = 5.3 +/- 0.43 nM,考虑受体数量摩尔浓度时为4.58 +/- 0.46 nM,与双嘧达莫一样显示出非竞争性机制。嗜铬细胞中存在的高亲和力受体的Kd = 6.8 +/- 0.8 nM,每个细胞的受体数量为630 000 +/- 40 000。