Chanal J L, Audran M, Bret M C, Cousse H, Fauran F, Rieu J P
Physical Laboratory, Faculté de Pharmacie, Montpellier, France.
Arzneimittelforschung. 1988 Oct;38(10):1454-60.
Metbufen, II, itanoxone, I, and two other derivatives of gamma-aryl-gamma-keto-substituted butyric acids labelled with 14C in their carbonyl group were synthesized for a metabolic investigation in rats. Profound changes in pharmacokinetic parameters, most specifically in the distribution, elimination, and metabolic pathways, were induced by substitution in the aromatic nucleus or changes in saturation of the aliphatic chain. The metabolites isolated from plasma and urine were identified by gas chromatography and mass spectrometry, by comparison with chemical controls, revealing the processes of metabolism of these structural analogues. This difference in metabolism further understanding of the diversity of biological effects inherent in these compounds.
合成了美布洛芬（Metbufen）II、伊他诺酮（itanoxone）I以及另外两种羰基标记有¹⁴C的γ-芳基-γ-酮取代丁酸衍生物，用于在大鼠体内进行代谢研究。芳环上的取代或脂肪链饱和度的改变会引起药代动力学参数的显著变化，最明显的是分布、消除和代谢途径方面的变化。通过气相色谱和质谱，并与化学对照品比较，鉴定了从血浆和尿液中分离出的代谢产物，揭示了这些结构类似物的代谢过程。代谢方面的这种差异进一步加深了对这些化合物固有生物效应多样性的理解。
