Antiplatelet effects of R,S-(meso)-alpha, alpha'-bis[3-(N,N-diethylcarbamoyl) piperidino]-p-xylene ex vivo in the dog and in vivo in the mouse.

Antiplatelet effects of R,S-(meso)-alpha, alpha'-bis[3-(N,N-diethylcarbamoyl) piperidino]-p-xylene ex vivo in the dog and in vivo in the mouse.
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R,S-(内消旋)-α,α-双[3-(N,N-二乙基氨基甲酰基)哌啶基]-对二甲苯在狗离体和小鼠体内的抗血小板作用。

DOI:
10.1016/s0306-3623(96)00272-8
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发表时间:
1997
期刊:
General pharmacology
影响因子:
--
通讯作者:
Gollamudi,R
Gollamudi,R
中科院分区:
--
文献类型:
--
作者:
Han,G;Bannerman,D;Handa,RK;Dillingham,EO;Lawrence,WH;Gollamudi,R

文献摘要

相似文献

1. 尼培他胺α, α′-双[3-(N, N-二乙基氨基甲酰基)哌啶]-对二甲苯(a -1)是一种血小板聚集抑制剂。中位异构体A-1c在抑制狗体内胶原诱导的血小板聚集方面,在效力和持续时间上优于由R, R-, S, S-和R, S-(中位异构体)组成的合成非对映异构体混合物。2. 在保护小鼠免受胶原+肾上腺素引起的血栓栓塞性死亡方面,A-1c也比A-1更有效,作用时间更长。3. 这种化合物的抗血小板作用机制似乎与它能够防止激动剂诱导的血小板环腺苷单磷酸(cAMP)水平的抑制有关。
1. The nipecotamide alpha, alpha'-bis [3-(N, N-diethylcarbamoyl) piperidino]-p-xylene (A-1) is a platelet aggregation inhibitor. The meso diastereomer A-1c is superior in potency and duration to the synthetic diastereomeric mixture consisting of the R, R-, S, S-, and R, S-(meso) isomers in inhibiting collagen-induced platelet aggregation ex vivo in the dog. 2. A-1c also is more potent and longer acting than A-1 in protecting mice from collagen+ epinephrine-induced thromboembolic death. 3. The mechanism of antiplatelet action of this compound appears to be related to its ability to prevent agonist-induced inhibition of platelet cyclic adenosine monophosphate (cAMP) levels.