5'-二磷酸腺苷诱导的人血小板聚集受到5'-单磷酸腺苷和5'-三磷酸腺苷的2-烷硫基类似物的特异性而非竞争性抑制。
Specific but noncompetitive inhibition by 2-alkylthio analogues of adenosine 5'-monophosphate and adenosine 5'-triphosphate of human platelet aggregation induced by adenosine 5'-diphosphate.
作者信息
Cusack N J, Hourani S M
出版信息
Br J Pharmacol. 1982 Feb;75(2):397-400. doi: 10.1111/j.1476-5381.1982.tb08800.x.
Abstract
Some 2-alkylthio derivatives of adenosine 5'-monophosphate (AMP), adenosine 5'-monophosphorothioate (AMPS) and adenosine 5'-triphosphate (ATP) were examined as inhibitors of human platelet aggregation. 2-Methylthio-AMP, 2-ethylthio-AMP, 2-(pentan-l-yl)thio-AMP, 2-ethylthio-AMPS, 2-methylthio-ATP and 2-ethylthio-ATP (100 microM) each inhibited aggregation induced by adenosine 5'-diphosphate (ADP) but not by 11 alpha, 9 alpha-epoxymethano prostaglandin H2, a stable endoperoxide analogue. Log dose-response curves to ADP in the absence and presence of each inhibitor were not parallel and the inhibition could not be overcome by high concentrations of ADP. The ATP analogues achieved greater inhibition of aggregation induced by ADP (5 microM) than did the AMP analogues. The order of potency of the AMP analogues was 2-ethylthio-AMPS greater than 2-ethylthio-AMP greater than 2-(pentan-l-yl)thio-AMP greater than 2-methylthio-AMP, and 2-methylthio-ATP was more potent than 2-ethylthio-ATP. These 2-alkylthio substituted analogues of AMP and ATP are specific but noncompetitive inhibitors of ADP-induced human platelet aggregation.
摘要
研究了5'-单磷酸腺苷（AMP）、5'-单磷酸腺苷硫代磷酸酯（AMPS）和5'-三磷酸腺苷（ATP）的一些2-烷硫基衍生物作为人血小板聚集抑制剂的作用。2-甲硫基-AMP、2-乙硫基-AMP、2-（戊-1-基）硫基-AMP、2-乙硫基-AMPS、2-甲硫基-ATP和2-乙硫基-ATP（100微摩尔）均抑制由5'-二磷酸腺苷（ADP）诱导的聚集，但不抑制11α，9α-环氧甲撑前列腺素H2（一种稳定的内过氧化物类似物）诱导的聚集。在不存在和存在每种抑制剂的情况下，对ADP的对数剂量-反应曲线不平行，且高浓度的ADP不能克服这种抑制作用。ATP类似物对ADP（5微摩尔）诱导的聚集的抑制作用比AMP类似物更强。AMP类似物的效力顺序为2-乙硫基-AMPS＞2-乙硫基-AMP＞2-（戊-1-基）硫基-AMP＞2-甲硫基-AMP，且2-甲硫基-ATP比2-乙硫基-ATP更有效。这些AMP和ATP的2-烷硫基取代类似物是ADP诱导的人血小板聚集的特异性非竞争性抑制剂。
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