DIPYRIDAMOLE INHIBITION OF ADENOSINE METABOLISM IN HUMAN-BLOOD
DIPYRIDAMOLE INHIBITION OF ADENOSINE METABOLISM IN HUMAN-BLOOD
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DOI：
10.1016/0014-2999(83)90026-2
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发表时间：
1983-01-01
影响因子：
5
通讯作者：
KLABUNDE, RE
中科院分区：
文献类型：
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作者：
KLABUNDE, RE
研究了双嘧达莫对人全血中腺苷代谢的影响。通过将[3H]腺苷添加到在37℃下孵育的血液中来测定腺苷消失以及脱氨基和磷酸化产物的形成的半衰期。 C.初始腺苷浓度为10 nmol/血液。添加标记的腺苷后，在特定时间取出等份血液。随后通过反相高压液相色谱分析等分试样的腺苷及其产物。未稀释血液中腺苷的半衰期<10秒；因此，为了准确评估双嘧达莫的作用，将血液用等渗盐水按1:12稀释。在此稀释度下，腺苷的半衰期为 1.3 分钟。 1 nmol/ml 血液中的双嘧达莫浓度引起 90% 的腺苷代谢抑制。在浓度 > 10 nmol/ml 血液时，抑制几乎完全，血浆脱氨除外。由于双嘧达莫的这些抑制浓度与在人类中治疗时达到的浓度处于同一数量级，因此这些数据表明治疗浓度的双嘧达莫引起全血中腺苷代谢的显着抑制。
The effects of dipyridamole on the metabolism of adenosine were studied in human whole blood. The half-life for adenosine disappearance and the formation of deamination and phosphorylation products were determined by adding [3H]adenosine to blood incubating at 37.degree. C. The initial adenosine concentration was 10 nmol/blood. Aliquots of blood were removed at specific times following the addition of labeled adenosine. The aliquots were later assayed for adenosine and its products by reverse-phase high pressure liquid chromatography. The half-life for adenosine in undiluted blood was < 10 s; therefore, to accurately evaluate the effects of dipyridamole, blood was diluted 1:12 in isotonic saline. At this dilution, the half-life for adenosine was 1.3 min. Dipyridamole concentrations of 1 nmol/ml blood caused 90% inhibition of adenosine metabolism. Inhibition was virtually complete, except for plasma deamination, at concentrations > 10 nmol/ml blood. Since these inhibitory concentrations of dipyridamole are on the same order as those achieved therapeutically in man, these data indicate that dipyridamole at therapeutic concentrations causes significant inhibition of adenosine metabolism in whole blood.