Chahine R, Cheav S L
Centre de recherche, Hôpital du Sacré-Coeur de Montréal, Québec, Canada.
Arzneimittelforschung. 1991 Apr;41(4):449-52.
Glycerolformal (CAS 5464-28-8; a mixture of 1,3-dioxan-5-ol and 1,3-dioxolane-4-methanol) used as an organic solvent or vehicle for drugs has been shown to possess its own toxicopharmacological activities. The aim of the present investigation was to determine the effects of glycerolformal on sympathetic neurotransmission in the isolated rabbit heart. At concentrations between 0.05 and 1 mmol/l glycerolformal inhibits both the neuronal and extraneuronal uptake of noradrenaline and its metabolism degradation which could explain the initial positive inotropic action of glycerolformal on the heart by increasing noradrenaline concentration in the synaptic cleft. However, the preponderant effect of glycerolformal was an inhibition of noradrenaline release, resulting in a myocardial depression which may explain the hypotension observed in the anesthetized rat. Hence, it is important to take into account the interference effects of glycerolformal with other molecules, when used as solvent or vehicle for drugs.
作为药物的有机溶剂或载体使用的甘油甲醛（CAS 5464-28-8；1,3-二氧六环-5-醇和1,3-二氧戊环-4-甲醇的混合物）已被证明具有自身的毒理药理活性。本研究的目的是确定甘油甲醛对离体兔心脏交感神经传递的影响。在0.05至1 mmol/l的浓度范围内，甘油甲醛抑制去甲肾上腺素的神经元和神经元外摄取及其代谢降解，这可以通过增加突触间隙中去甲肾上腺素的浓度来解释甘油甲醛对心脏最初的正性肌力作用。然而，甘油甲醛的主要作用是抑制去甲肾上腺素的释放，导致心肌抑制，这可能解释了在麻醉大鼠中观察到的低血压。因此，当甘油甲醛用作药物的溶剂或载体时，考虑其对其他分子的干扰作用很重要。
