Damaj M I, Trouvin J H, Lambrey B, Jacquot C
Laboratoire de Pharmacologie et de Pharmacocinétique, Faculté de Pharmacie, Chatenay-Malabry, France.
J Pharm Sci. 1990 Jun;79(6):516-8. doi: 10.1002/jps.2600790612.
5-(1'-Phenyl-4'-piperazinomethyl)-2-amino-2-oxazoline (1; COR3224), a derivative of 2-amino-2-oxazolines with antidepressant properties in rats, was assayed in plasma by high-performance liquid chromatography. After back extraction, 1 and a ortho-O-methyl derivative of 1 as the internal standard were separated by reversed-phase liquid chromatography and measured by UV detection (235 nm). The method is rapid and specific: the detection was linear in the range 125-1000 micrograms.L-1, with a detection limit of 50 micrograms.L-1. This method allowed the determination of pharmacokinetic parameters in six beagle dogs after intravenous and oral administration of 14C-labeled 1 ([14C]1) in a crossover study. The comparison of the results obtained from total radioactivity counting and unchanged product evaluated by HPLC-UV suggest the presence of metabolites.
5-(1'-苯基-4'-哌嗪甲基)-2-氨基-2-恶唑啉（1；COR3224）是一种在大鼠中具有抗抑郁特性的2-氨基-2-恶唑啉衍生物，采用高效液相色谱法在血浆中进行测定。经过反萃取后，1及其邻位-O-甲基衍生物作为内标物，通过反相液相色谱法分离，并通过紫外检测（235nm）进行测定。该方法快速且特异：检测在125 - 1000μg·L⁻¹范围内呈线性，检测限为50μg·L⁻¹。在一项交叉研究中，该方法可用于测定六只比格犬静脉注射和口服¹⁴C标记的1（[¹⁴C]1）后的药代动力学参数。通过总放射性计数获得的结果与通过高效液相色谱 - 紫外法评估的未变化产物进行比较，表明存在代谢物。
