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1
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.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。
Br J Pharmacol. 1982 Feb;75(2):397-400. doi: 10.1111/j.1476-5381.1982.tb08800.x.
2
Competitive inhibition by adenosine 5'-triphosphate of the actions on human platelets of 2-chloroadenosine 5'-diphosphate, 2-azidoadenosine 5'-diphosphate and 2-methylthioadenosine 5'-diphosphate.5'-三磷酸腺苷对2-氯-5'-二磷酸腺苷、2-叠氮基-5'-二磷酸腺苷和2-甲硫基-5'-二磷酸腺苷作用于人类血小板的竞争性抑制作用。
Br J Pharmacol. 1982 Oct;77(2):329-33. doi: 10.1111/j.1476-5381.1982.tb09302.x.
3
Inhibition of ADP-induced platelet aggregation by adenosine tetraphosphate.四磷酸腺苷对二磷酸腺苷诱导的血小板聚集的抑制作用。
Thromb Haemost. 1976 Nov 30;36(2):388-91.
4
Effects of analogues of adenine nucleotides on increases in intracellular calcium mediated by P2T-purinoceptors on human blood platelets.腺嘌呤核苷酸类似物对人血小板上P2T嘌呤受体介导的细胞内钙增加的影响。
Br J Pharmacol. 1993 Mar;108(3):728-33. doi: 10.1111/j.1476-5381.1993.tb12869.x.
5
Inhibition by a stable analogue of adenosine triphosphate of platelet aggregation by adenosine diphosphate.三磷酸腺苷的一种稳定类似物对二磷酸腺苷诱导的血小板聚集的抑制作用。
Br J Pharmacol. 1977 Sep;61(1):87-9. doi: 10.1111/j.1476-5381.1977.tb09743.x.
6
Leukocyte count and leukocyte ecto-nucleotidase are major determinants of the effects of adenosine triphosphate and adenosine diphosphate on platelet aggregation in human blood.白细胞计数和白细胞外核苷酸酶是三磷酸腺苷和二磷酸腺苷对人血中血小板聚集作用的主要决定因素。
Platelets. 2005 May-Jun;16(3-4):159-70. doi: 10.1080/09537100500063889.
7
Potentiation of adenosine triphosphate-induced contractile responses of the guinea-pig isolated vas deferens by adenosine monophosphate and adenosine 5'-monophosphorothioate.单磷酸腺苷和5'-硫代磷酸腺苷对豚鼠离体输精管三磷酸腺苷诱导的收缩反应的增强作用。
Br J Pharmacol. 1987 Jul;91(3):633-9. doi: 10.1111/j.1476-5381.1987.tb11257.x.
8
Role of extracellular ATP metabolism in regulation of platelet reactivity.细胞外ATP代谢在调节血小板反应性中的作用。
J Lab Clin Med. 2002 Sep;140(3):166-75. doi: 10.1067/mlc.2002.126719.
9
Differential effects of adenine nucleotide analogues on shape change and aggregation induced by adnosine 5-diphosphate (ADP) in human platelets.腺嘌呤核苷酸类似物对人血小板中5-二磷酸腺苷（ADP）诱导的形态变化和聚集的不同作用。
Br J Pharmacol. 1999 Jul;127(6):1359-66. doi: 10.1038/sj.bjp.0702690.
10
Rat platelet aggregation by ATP. Aggregometrical and ultrastructural comparison with aggregations induced by ADP and collagen.ATP诱导的大鼠血小板聚集。与ADP和胶原蛋白诱导的聚集进行聚集测定和超微结构比较。
Am J Pathol. 1976 Dec;85(3):581-94.

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Blood cells: an historical account of the roles of purinergic signalling.血细胞：嘌呤能信号传导作用的历史记述
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Racial differences in resistance to P2Y12 receptor antagonists in type 2 diabetic subjects.2型糖尿病患者对P2Y12受体拮抗剂抵抗的种族差异。
J Pharmacol Exp Ther. 2014 Oct;351(1):33-43. doi: 10.1124/jpet.114.215616. Epub 2014 Jul 22.
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The novel suramin analogue NF864 selectively blocks P2X1 receptors in human platelets with potency in the low nanomolar range.新型苏拉明类似物NF864在低纳摩尔范围内有效选择性阻断人血小板中的P2X1受体。
Naunyn Schmiedebergs Arch Pharmacol. 2005 Jul;372(1):1-13. doi: 10.1007/s00210-005-1085-z. Epub 2005 Sep 13.
4
Differential effects of adenine nucleotide analogues on shape change and aggregation induced by adnosine 5-diphosphate (ADP) in human platelets.腺嘌呤核苷酸类似物对人血小板中5-二磷酸腺苷（ADP）诱导的形态变化和聚集的不同作用。
Br J Pharmacol. 1999 Jul;127(6):1359-66. doi: 10.1038/sj.bjp.0702690.
5
Effects of analogues of adenine nucleotides on increases in intracellular calcium mediated by P2T-purinoceptors on human blood platelets.腺嘌呤核苷酸类似物对人血小板上P2T嘌呤受体介导的细胞内钙增加的影响。
Br J Pharmacol. 1993 Mar;108(3):728-33. doi: 10.1111/j.1476-5381.1993.tb12869.x.
6
Characterization of the effects of 2-methylthio-ATP and 2-chloro-ATP on brain capillary endothelial cells: similarities to ADP and differences from ATP.2-甲硫基三磷酸腺苷和2-氯三磷酸腺苷对脑毛细血管内皮细胞作用的特征：与二磷酸腺苷的相似性及与三磷酸腺苷的差异
Br J Pharmacol. 1994 Jul;112(3):775-80. doi: 10.1111/j.1476-5381.1994.tb13146.x.
7
FPL 66096: a novel, highly potent and selective antagonist at human platelet P2T-purinoceptors.FPL 66096：一种新型的、高效且具有选择性的人血小板P2T嘌呤受体拮抗剂。
Br J Pharmacol. 1994 Nov;113(3):1057-63. doi: 10.1111/j.1476-5381.1994.tb17100.x.
8
Pharmacological profile of the novel P2T-purinoceptor antagonist, FPL 67085 in vitro and in the anaesthetized rat in vivo.新型P2T嘌呤受体拮抗剂FPL 67085的体外和麻醉大鼠体内药理学特性
Br J Pharmacol. 1995 Jul;115(6):1110-6. doi: 10.1111/j.1476-5381.1995.tb15925.x.
9
Competitive inhibition by adenosine 5'-triphosphate of the actions on human platelets of 2-chloroadenosine 5'-diphosphate, 2-azidoadenosine 5'-diphosphate and 2-methylthioadenosine 5'-diphosphate.5'-三磷酸腺苷对2-氯-5'-二磷酸腺苷、2-叠氮基-5'-二磷酸腺苷和2-甲硫基-5'-二磷酸腺苷作用于人类血小板的竞争性抑制作用。
Br J Pharmacol. 1982 Oct;77(2):329-33. doi: 10.1111/j.1476-5381.1982.tb09302.x.
10
Adenosine 5-diphosphate antagonists and human platelets: no evidence that aggregation and inhibition of stimulated adenylate cyclase are mediated by different receptors.腺苷5-二磷酸拮抗剂与人类血小板：无证据表明聚集和刺激型腺苷酸环化酶的抑制作用由不同受体介导。
Br J Pharmacol. 1982 May;76(1):221-7. doi: 10.1111/j.1476-5381.1982.tb09210.x.

本文引用的文献

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Aggregation of blood platelets by adenosine diphosphate and its reversal.二磷酸腺苷引起的血小板聚集及其逆转
Nature. 1962 Jun 9;194:927-9. doi: 10.1038/194927b0.
2
2-methylthioadenosine-5'-phosphate: a specific inhibitor of platelet aggregation.2-甲硫基腺苷-5'-磷酸：血小板聚集的特异性抑制剂。
Nature. 1969 Jun 14;222(5198):1073-4. doi: 10.1038/2221073a0.
3
Effect of the rapid shape change of platelets on the transmission and scattering of light through plasma.血小板快速形状变化对光在血浆中传播和散射的影响。
Nat New Biol. 1971 Jun 16;231(24):220-2. doi: 10.1038/newbio231220a0.
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Platelet aggregation inhibitors. 7. S-substituted 2-thioadenosine 5'-monophosphates.血小板聚集抑制剂。7. S-取代的2-硫代腺苷5'-单磷酸酯。
J Med Chem. 1973 Dec;16(12):1389-91. doi: 10.1021/jm00270a015.
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Platelet aggregation inhibitors. 6. 2-Thioadenosine derivatives.血小板聚集抑制剂。6. 2-硫代腺苷衍生物。
J Med Chem. 1973 Dec;16(12):1381-8. doi: 10.1021/jm00270a014.
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Three new adenosine triphosphate analogs. Synthesis and effects on isolated gut.三种新型三磷酸腺苷类似物。合成及其对离体肠道的作用。
J Med Chem. 1973 Oct;16(10):1188-90. doi: 10.1021/jm00268a028.
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Interactions of the pharmacological receptors of blood platelets with adenylate cyclase.血小板的药理受体与腺苷酸环化酶的相互作用。
Ser Haematol. 1973;6(3):333-50.
8
Inhibition of platelet aggregation and the platelet release reaction by alpha, omega diadenosine polyphosphates.α,ω-二腺苷多磷酸盐对血小板聚集和血小板释放反应的抑制作用。
FEBS Lett. 1975 Jun 1;54(1):57-60. doi: 10.1016/0014-5793(75)81067-2.
9
Inhibition of ADP-induced platelet aggregation by adenosine tetraphosphate.四磷酸腺苷对二磷酸腺苷诱导的血小板聚集的抑制作用。
Thromb Haemost. 1976 Nov 30;36(2):388-91.
10
Platelet aggregation inhibitors. IX. Chemical transformation of adenosine into 2-thioadenosine derivatives.血小板聚集抑制剂。IX。腺苷向2-硫代腺苷衍生物的化学转化。
Chem Pharm Bull (Tokyo). 1977 Aug;25(8):1959-69. doi: 10.1248/cpb.25.1959.

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.

DOI:10.1111/j.1476-5381.1982.tb08800.x
PMID:7186826
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2071616/
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。