新型二肽神经保护剂在大鼠体内的代谢。

Metabolism of a New Dipeptide Neuroprotector in Rats.

机构信息

Laboratory of Pharmacokinetics, V. V. Zakusov Research Institute of Pharmacology, Moscow, Russia.

出版信息

Bull Exp Biol Med. 2022 Mar;172(5):579-582. doi: 10.1007/s10517-022-05440-3. Epub 2022 Mar 30.

Abstract

Metabolism of a new neuroprotector GZK-111 (N-phenylacetylglycyl-L-proline ethyl ester) in rat blood plasma was studied by HPLC-mass spectrometry. Four biotransformation products were identified. It is concluded that the main ways of GZK-111 biotransformation are hydrolysis of the ester bond by esterases followed by degradation of the resulting metabolite, as well as reactions leading to the formation of phenylacetic acid and cycloprolylglycine that exhibits neuropsychotropic activity.

摘要

采用高效液相色谱-质谱联用法研究了新型神经保护剂 GZK-111（N-苯乙酰甘氨酰-L-脯氨酸乙酯）在大鼠血浆中的代谢情况。鉴定出 4 种生物转化产物。研究结果表明，GZK-111 的主要生物转化途径是通过酯酶水解酯键，然后降解生成的代谢物，以及导致形成具有神经精神活性的苯乙酸和环丙基甘氨酸的反应。