Cheav S L, Chahine R, Mroué M S
Laboratoire de Pharmacodynamie, Unité de Formation et de Recherche de Pharmacie, France.
Arzneimittelforschung. 1992 Aug;42(8):997-1000.
Glycerol formal (CAS 5464-28-8), an organic solvent used to vehicle drugs to target cells, has been shown to possess its own toxicopharmacological properties. The present work was undertaken to study its direct effect on the isolated rabbit heart. At 2.3 and 4.6 mmol/l (bolus) glycerol formal exerted a positive inotropic effect. Upon a perfusion of 4.5 mmol/l/h, the left ventricular pressure and the coronary flow were increased, while at 11 mmol/l/h these two parameters showed a tendency to decrease. Glycerol formal upon a perfusion at 11 mmol/l/h decreased mildly the positive inotropic effect of noradrenaline, and strongly that produced by acetylcholine at a nicotinic dose, while it accentuated the bradycardia induced by acetylcholine at a muscarinic dose. On the contrary it potentiated the stimulant effect of nicotine. The positive inotropic effects of tyramine, dimethylphenylpiperazinium and potassium chloride were decreased showing an inhibition of noradrenaline liberation induced by glycerol formal at the doses used. The action of glycerol formal on agents inducing a positive inotropic effect, except nicotine, and its cardiodepressant effect are probably partly due to its action on the Ca2+ ion.
甲醛缩甘油（化学物质登记号5464-28-8）是一种用于将药物运载至靶细胞的有机溶剂，已被证明具有自身的毒理学特性。本研究旨在探讨其对离体兔心脏的直接作用。在2.3和4.6毫摩尔/升（推注）时，甲醛缩甘油产生正性肌力作用。当以4.5毫摩尔/升/小时的速度灌注时，左心室压力和冠状动脉血流量增加，而在11毫摩尔/升/小时时，这两个参数呈下降趋势。以11毫摩尔/升/小时的速度灌注时，甲醛缩甘油轻度降低去甲肾上腺素的正性肌力作用，强烈降低烟碱剂量的乙酰胆碱所产生的正性肌力作用，而它增强毒蕈碱剂量的乙酰胆碱所诱发的心动过缓。相反，它增强尼古丁的刺激作用。酪胺、二甲基苯基哌嗪鎓和氯化钾的正性肌力作用降低，表明在所使用的剂量下，甲醛缩甘油抑制去甲肾上腺素的释放。甲醛缩甘油对除尼古丁外的具有正性肌力作用的药物的作用及其心脏抑制作用可能部分归因于其对钙离子的作用。
