摘要
用比浊法和放射免疫法分别测定盐酸非洛普对兔和人血小板聚集及兔血栓素Ａ２（ＴＸＡ２）和动脉壁前列环素（ＰＧＩ２）含量的影响。盐酸非洛普呈剂量依赖性抑制ＡＤＰ（ＩＣ５０＝５．８×１０－４ｍｏｌ·Ｌ－１）和ＡＡ诱导的兔血小板聚集。对ＡＤＰ和Ａｄｒ诱导的人血小板聚集亦有明显抑制作用且呈剂量依赖性，ＩＣ５０值分别为１．２和１．３×１０－４ｍｏｌ·Ｌ－１。盐酸非洛普短期应用（８ｍｇ·ｋｇ－１ｉｖｔｉｄ×２ｄ）明显抑制ＡＤＰ和ＡＡ诱导的兔血小板聚集及ＴＸＢ２的产生和释放，对兔动脉壁和血浆６－ｋｅｔｏ－ＰＧＦ１α含量无显著影响。研究结果表明，盐酸非洛普抗血小板聚集作用与其抑制血小板ＴＸＡ２合成和释放有关，亦可能与其α２受体阻断作用有关。
The effects of DDPH on human and rabbit platelets aggregation and its mecha nisms were investigated. DDPH produced a dose-dependent inhibiton of rabbit platelets aggregation by ADP (IC50=5.8×10-4mol·L-1)and archidonic acid(AA). The human platelet aggregation induced by ADP and adrenaline (Adr) was inhibited by DDPH with IC50 value of 1.2 and 1.3×10-4 mol·L-1, respectively.The rabbit platelet aggregation induced by ADP and AA was inhibited with DDPH in vivo.DDPH(8 mg·kg-1 iv, 3 times/day×2) decreased TXB2 concentration in rabbit platelets and inhibited formation and release of TXB2 in activited rabbit platelets, but had no effect on concentration of 6-keto-PGF1α in plasma and arterial wall.The results indicate that DDPH has antiplatelet aggregation effect and its mechanisms may be relsted to the inhibition of platelet TXA2 formation and release,probably also to its adrenoreceptors blocking effect.
出处
《中国药理学通报》
CAS
CSCD
北大核心
1996年第3期251-253,共3页
Chinese Pharmacological Bulletin
关键词
盐酸非洛普
血小板聚集
血栓素A2
前列环素
DDPH
platelet aggregation
TXA_2
PGI_2
turbidithetry
radioimmunoassay
