Relationships between chemical structure and inhibition of ADP-stimulated human thrombocyte release of serotonin and platelet factor 4.

Relationships between chemical structure and inhibition of ADP-stimulated human thrombocyte release of serotonin and platelet factor 4.
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化学结构与 ADP 刺激的人血小板释放血清素和血小板因子 4 的抑制之间的关系。

DOI:
10.1016/s0304-4165(89)80023-6
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发表时间:
1989
期刊:
Biochimica et biophysica acta
影响因子:
--
通讯作者:
Gollamudi,R
Gollamudi,R
中科院分区:
--
文献类型:
--
作者:
Dillingham,EO;Lasslo,A;Carter-Burks,G;Bond,SE;Gollamudi,R

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本文研究了氨基甲酰哌啶烷和N-烷基哌啶甲酰基哌嗪衍生物对二磷酸腺苷(ADP)诱导的人血小板聚集、5-羟色胺(5-HT)释放和血小板第四因子(PF-4)释放的抑制作用。该程序旨在允许同时测定所有三组值。大多数化合物在阻断PF-4方面的效力超过两倍(X = 91 ± 1(S.E.,n= 1)%)与其对5-HT的抑制作用(X= 38 ± 1(SE,n= 6)%)释放;未能满足这些标准的一种化合物在阻止PF-4释放方面仍然明显比5-HT更强。由于化合物的血小板聚集抑制值与其5-HT释放阻断效力在相同范围内,但在阻止PF-4释放方面具有显著更大的影响,因此表明血小板质膜和包裹致密体的衬里可能具有某些共性,而包裹α颗粒的鞘可能以有形的方式不同于两者。
The inhibitory potencies of carbamoylpiperidinoalkane andN-alkylnipecotoylpiperazine derivatives on ADP-stimulated human blood platelet aggregation, serotonin (5-HT) release and platelet factor 4 (PF-4) release were evaluated. The procedure was designed to allow concurrent determination of all three sets of values. Most compounds were more than twice as potent in blocking PF-4 (X = 91 ± 1(S.E.,n= 1)%) compared to their inhibition of 5-HT (X= 38 ± 1(S.E.,n= 6)%) release; the one compound which failed to meet these criteria was still decidedly more powerful in impeding PF-4 than 5-HT release. Since the compounds' platelet aggregation-inhibitory values were within the same range as their 5-HT release-blocking potencies, but had a strikingly greater impact in arresting PF-4 release, it is suggested that the platelet plasma membrane and the lining enveloping the dense bodies may share certain commonalities, while the sheathing encasing theα-granules may differ from both in a tangible manner.
β-血栓球蛋白 (β-TG) 和血小板因子 4 (PF4) 通过二磷酸腺苷 (ADP) 与天然全血接触而释放。
DOI: 10.1016/0049-3848(85)90247-6
发表时间: 1985
影响因子: 7.5
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DOI: 10.1016/0049-3848(82)90278-x
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影响因子: 7.5
作者:
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人血小板因子 4:亚细胞定位和完整血小板释放的特征。
DOI: 10.1016/0049-3848(80)90366-7
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血小板 5-羟色胺系统:生理学和病理生理学。
DOI: --
发表时间: 1987
影响因子: 3.5
作者:
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DOI: 10.1161/01.res.42.3.402
发表时间: 1978-01-01
影响因子: 20.1
作者:
WITTE, LD;KAPLAN, KL;GOODMAN, DS
通讯作者: GOODMAN, DS