Marvola M
Acta Pharmacol Toxicol (Copenh). 1977 Jan;40(1):22-32. doi: 10.1111/j.1600-0773.1977.tb02050.x.
To study how acetylation affects the activity of sympathomimetic amines the effects of tyramine, amphetamine, ephedrine, phenylephrine, orciprenaline and salbutamol and of their O- and N-acetyl derivatives on blood glucose and free fatty acid concentrations were studied in the rabbit. Hyperglycemia was induced by all parent compounds except amphetamine which tended to have a weak hypoglycaemic action. Hyperlipaemia in the doses used was induced by ephedrine and orciprenaline but not by the other parent compounds. Usually acetylation decreased the metabolic effects of the compounds but O-acetylation of tyramine and salbutamol caused hyperlipaemia and O-acetylation of ephedrine increased its fatty acid-mobilizing action, perhaps as a consequence of increased lipid solubility of the compounds. The ultimate effects of the O-acetyl derivatives were probably at least partly due to deacetylation at their sites of action. However O-acetylation of sympathomimetics could perhaps be used to induce drug latentiation.
为研究乙酰化如何影响拟交感胺的活性，在兔身上研究了酪胺、苯丙胺、麻黄碱、去氧肾上腺素、间羟异丙肾上腺素和沙丁胺醇及其O-和N-乙酰衍生物对血糖和游离脂肪酸浓度的影响。除苯丙胺往往有较弱的降血糖作用外，所有母体化合物均诱导了高血糖症。所用剂量的高脂血症由麻黄碱和间羟异丙肾上腺素诱导，而非其他母体化合物。通常乙酰化降低了化合物的代谢作用，但酪胺和沙丁胺醇的O-乙酰化导致了高脂血症，麻黄碱的O-乙酰化增加了其脂肪酸动员作用，这可能是由于化合物脂溶性增加的结果。O-乙酰衍生物的最终作用可能至少部分归因于其作用部位的脱乙酰化。然而，拟交感神经药的O-乙酰化或许可用于诱导药物潜伏化。
