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本文观察了阿片类物质影响体外培养心肌细胞搏动功能的生化机制。发现阿片物质对心肌细胞的直接作用机制涉及胞内[Ca~(2+)]i浓度和腺苷酸环化酶(AC)活性改变的调节,方式较复杂。广谱型阿片受体激动剂(κ-δ-μ)依托啡促进外钙内流和内钙释放,增加心肌细胞内[Ca~(2+)]i,其他一些阿片物质则未发现此种作用,吗啡,甲硫脑啡肽对AC活性具有双相调节;强啡肽,β-内啡肽则表现为刺激AC活性。AC活性改变受G蛋白亚基Gi和Gs的共同调控,但以Gs为主。
This article investigates the biochemical mechanisms by which opioids affect cardiomyocyte pulsatility in vitro. It was found that the direct mechanism of action of opioids on cardiomyocytes involves the regulation of [Ca ~ (2 +)] i concentration and the change of adenylyl cyclase (AC) activity in a complex way. Broad-spectrum opioid receptor agonist (κ-δ-μ) retentate promotes extracellular calcium influx and intracellular calcium release, increasing [Ca 2+] i in cardiomyocytes but not in other opioids Morphine and methyl-thio-enkephalin have biphasic regulation of AC activity, while dynorphin and β-endorphin are shown to stimulate AC activity. AC activity changes by the G protein subunits Gi and Gs co-regulation, but mainly Gs.