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[具有促智活性的吡拉西坦二肽类似物GVS-111及其主要代谢产物的药代动力学]

[The pharmacokinetics of the dipeptide analog of piracetam with nootropic activity GVS-111 and of its basic metabolites].

作者信息

Boĭko S S, Zherdev V P, Dvorianinov A A, Gudasheva T A, Ostrovskaia R U, Voronina T A, Rozantsev G G, Seredenin S B

出版信息

Eksp Klin Farmakol. 1997 Mar-Apr;60(2):53-5.

PMID:9206571
Abstract

The pharmacokinetics of a new nootropic dipeptide analog of piracetam-N-phenylacetyl-L-prolylglycine (GWS-111) and its main metabolites were studied in rats by means of high performance liquid chromatography and gas-liquid chromatography. The compound under study showed a greater resistance to an enzymatic effect than natural neuropeptides. In addition to an unchanged compound three of its metabolites were found in the blood plasma of the rats. One of them, cyclo-Pro-Gly was an active metabolite of GWS-111.

摘要

通过高效液相色谱法和气液色谱法,在大鼠体内研究了一种新型促智二肽类似物——吡拉西坦-N-苯乙酰-L-脯氨酰甘氨酸(GWS-111)及其主要代谢产物的药代动力学。与天然神经肽相比,所研究的化合物对酶作用表现出更大的抗性。除了未发生变化的化合物外,在大鼠血浆中还发现了其三种代谢产物。其中一种,环脯氨酰甘氨酸是GWS-111的活性代谢产物。

相似文献

1
[The pharmacokinetics of the dipeptide analog of piracetam with nootropic activity GVS-111 and of its basic metabolites].[具有促智活性的吡拉西坦二肽类似物GVS-111及其主要代谢产物的药代动力学]
Eksp Klin Farmakol. 1997 Mar-Apr;60(2):53-5.
2
The major metabolite of dipeptide piracetam analogue GVS-111 in rat brain and its similarity to endogenous neuropeptide cyclo-L-prolylglycine.二肽吡拉西坦类似物GVS-111在大鼠脑中的主要代谢产物及其与内源性神经肽环-L-脯氨酰甘氨酸的相似性。
Eur J Drug Metab Pharmacokinet. 1997 Jul-Sep;22(3):245-52. doi: 10.1007/BF03189814.
3
[The use of the HPLC method for the quantitative determination of a peptide analog of piracetam with nootropic activity and its main metabolites].[采用高效液相色谱法对具有促智活性的吡拉西坦肽类似物及其主要代谢物进行定量测定]
Eksp Klin Farmakol. 1996 Mar-Apr;59(2):38-40.
4
[Effect of the novel dipeptide nootropic agent noopept and its metabolite cyclo-L-prolylglycine on the transcallosal evoked potential in the rat brain].[新型二肽益智剂诺佩普及其代谢产物环-L-脯氨酰甘氨酸对大鼠脑胼胝体诱发电位的影响]
Eksp Klin Farmakol. 2002 Mar-Apr;65(2):3-5.
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[Design of the novel dipeptide neuropsychotropic drug preparations].[新型二肽神经精神药物制剂的设计]
Eksp Klin Farmakol. 2003 Mar-Apr;66(2):15-9.
6
Pharmacokinetics of new nootropic acylprolyldipeptide and its penetration across the blood-brain barrier after oral administration.
Bull Exp Biol Med. 2000 Apr;129(4):359-61. doi: 10.1007/BF02439270.
7
Proline-containing dipeptide GVS-111 retains nootropic activity after oral administration.含脯氨酸的二肽GVS-111口服后仍保留益智活性。
Bull Exp Biol Med. 2001 Oct;132(4):959-62. doi: 10.1023/a:1013663126973.
8
[The effect of the new nootropic dipeptide GVS-111 in different functional disorders of the escape reaction].新型益智二肽GVS-111对逃避反应不同功能障碍的影响
Eksp Klin Farmakol. 1998 May-Jun;61(3):10-2.
9
[Dipeptide nootropic agent GVS-111 prevents accumulation of the lipid peroxidation products during immobilization].二肽益智剂GVS-111可防止固定过程中脂质过氧化产物的积累
Eksp Klin Farmakol. 1997 Sep-Oct;60(5):15-8.
10
[Role of functional state of neuronal mitochondria of cerebral cortex in mechanisms of nootropic activity of neuroprotectors in rats with alloxan hyperglycemia].[大脑皮质神经元线粒体功能状态在四氧嘧啶性高血糖大鼠中神经保护剂促智活性机制中的作用]
Eksp Klin Farmakol. 2015;78(2):10-4.

引用本文的文献

1
Molecular Mechanism Underlying the Action of Substituted Pro-Gly Dipeptide Noopept.取代的脯氨酰-甘氨酸二肽诺肽普特作用的分子机制
Acta Naturae. 2016 Jan-Mar;8(1):82-9.