Pinacidil。临床调查。

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Pinacidil。临床调查。

药。1988;36增刊7:4-9。

PubMed ID

3076134 (在PubMed

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文摘

常规硫脲化合物的药理筛选选择了吡啶基氰基胍的降压效果。从这个氰基胍类化合物,1134页(pinacidil)是合成。Pinacidil具有不对称碳原子pinacolyl激进和(-)对映体比(+)更积极的对映体在体外和体内。Pinacidil口服后迅速吸收血浆浓度峰值的时间是0.5到1小时,延长释放配方,1 - 3和5 - 7小时。的抗高血压作用pinacidil剂量成正比。Pyridine-N-oxide主要代谢物和占大约一半的剂量在24小时内由尿排出。在高血压大鼠和狗,pinacidil的降血压效果存在剂量依赖的相关性和线性相关基线血压。血液动力学的概要文件的特点是增加心输出量体积增加中风的结果。心率的增加是减压反应。血压的下降之前,改按总外周阻力下降。 Preclinical haemodynamic studies suggest that pinacidil is a directly acting precapillary vasodilator. The resting membrane potential of smooth muscle cells is approximately -60mV whereas the equilibrium potential for potassium is more negative, between -80 and -90mV. Pinacidil opens K+ channels and allows potassium to attain its equilibrium potential, resulting in hyperpolarisation of the cell at rest. A hyperpolarised cell is less prone to depolarisation, and without depolarisation there is no activation of the voltage-operated Ca2+ channels and, hence, no muscle contraction.

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药物

Pinacidil