N-苯乙酰-L-脯氨酰甘氨酸乙酯

N-苯乙酰-L-脯氨酰甘氨酸乙酯
臨床資料
商品名（英语：Drug nomenclature）	Noopept
其他名稱	Omberacetam; GVS-111; DVD-111; SGS-111; benzylcarbonyl-Pro-Gly-OEt
法律規範狀態
法律規範	澳：限医生处方（S4）; 美：未批准的“新药（英语：Investigational New Drug）”（定义见《美国法典》第21卷第321(p)(1)条）。用于膳食补充剂、食品或药品不合法，其余不受管制;
识别信息
	IUPAC命名法 Ethyl 1-(phenylacetyl)-l-prolylglycinate; ;
CAS号	157115-85-0
PubChem CID	180496;
ChemSpider	157065 ;
UNII	4QBJ98683M;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID80166214 ;
化学信息
化学式	C17H22N2O4
摩尔质量	318.37 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES c2ccccc2CC(=O)N1CCC[C@@H]1C(=O)NCC(=O)OCC;
	InChI InChI=1S/C17H22N2O4/c1-2-23-16(21)12-18-17(22)14-9-6-10-19(14)15(20)11-13-7-4-3-5-8-13/h3-5,7-8,14H,2,6,9-12H2,1H3,(H,18,22)/t14-/m0/s1 ; Key:PJNSMUBMSNAEEN-AWEZNQCLSA-N ;

N-苯乙酰-l-脯氨酰甘氨酸乙酯（英語：N-Phenylacetyl-l-prolylglycine ethyl ester）被宣传为一种益智药，是环甘氨酸-脯氨酸（英语：Cyclic glycine-proline）（cGP）的前体药物^[1]。其他名称包括商品名Noopept（俄语：Ноопепт）^{[注 1]}、研发代号GVS-111和拟议国际非专有药名Omberacetam^[1]^[2]^[3]。

该药物的合成于1996年首次报道^[1]。它可以口服。截至2017年，其在人体内的代谢和消除半衰期尚不清楚^[1]。

该药物已被评估在治疗脑损伤和中风方面具有神经保护作用（英语：Neuroprotection）^[4]。

药理学

一项经常被引用的、最初用俄语发表的大鼠实验表明，Noopept通过“抗氧化作用、抗炎作用、抑制过量钙和谷氨酸的神經毒性以及改善血液流变性”发挥作用^[4]。大鼠研究表明，Noopept是内源性二肽环甘氨酸-脯氨酸（英语：Cyclic glycine-proline）的前体药物^[5]。环甘氨酸-脯氨酸是 AMPA受体（英语：AMPA receptor）的调节剂，其神经保护作用依赖于AMPA和TrkB受体（英语：Tropomyosin receptor kinase B）的激活^[6]。在细胞培养中，环甘氨酸-脯氨酸增加了脑源性神经营养因子（BDNF）^[7]。

一些研究表明，Noopept的药理特性源于其作为缺氧誘導因子（HIF-1）激活剂的作用^[8]^[9]。而HIF-1在多种人类癌症中过表达^[10]。

剂量

Noopept的常用剂量为每日10-30毫克。然而，尚无确凿证据表明任何剂量的Noopept是最佳的。针对Noopept的人体试验很少，一项荟萃分析指出，动物研究中的剂量范围在0.1mg/kg体重到10mg/kg体重之间^{[不可靠的醫學來源？]}^[11]。此外，尚无任何长期研究，评估以任何特定剂量长期服用Noopept的持久影响，最长的人体研究持续了56天^[12]。

参见

注释

^ 部分网站（页面存档备份，存于互联网档案馆）将Noopept翻译为诺普平，但并无官方来源依据。

参考来源

^ ^1.0 ^1.1 ^1.2 ^1.3 Noopept Information. Examine.com. [2017-04-06].
^ Proposed INN List 117. WHO Drug Information. 2017, 31 (2): 308 [2025-05-15]. （原始内容存档于2025-01-24）.
^ Omberacetam. AdisInsight. Springer Nature Switzerland AG. [2018-05-12]. （原始内容存档于2017-10-15）（英语）. Alternative Names: DVD-111; GVS 111; Noopept
^ ^4.0 ^4.1 Ostrovskaia RU, Gudasheva TA, Voronina TA, Seredenin SB. [The original novel nootropic and neuroprotective agent noopept]. Eksperimental'naia i Klinicheskaia Farmakologiia. 2002, 65 (5): 66–72. PMID 12596521 （俄语）.
^ Gudasheva TA, Boyko SS, Ostrovskaya RU, Voronina TA, Akparov VK, Trofimov SS, Rozantsev GG, Skoldinov AP, Zherdev VP, Seredenin SB. The major metabolite of dipeptide piracetam analogue GVS-111 in rat brain and its similarity to endogenous neuropeptide cyclo-L-prolylglycine. European Journal of Drug Metabolism and Pharmacokinetics. 1997, 22 (3): 245–252. PMID 9358206. doi:10.1007/BF03189814.
^ Gudasheva TA, Koliasnikova KN, Alyaeva AG, Nikolaev SV, Antipova TA, Seredenin SB. Neuroprotective Effect of the Neuropeptide Cycloprolylglycine Depends on AMPA- and TrkB-Receptor Activation. Doklady. Biochemistry and Biophysics. 2022-12, 507 (1): 264–267. PMID 36786983. doi:10.1134/S1607672922060047.
^ Gudasheva TA, Koliasnikova KN, Antipova TA, Seredenin SB. Neuropeptide cycloprolylglycine increases the levels of brain-derived neurotrophic factor in neuronal cells. Doklady. Biochemistry and Biophysics. 2016-07, 469 (1): 273–276. PMID 27599510. S2CID 254426990. doi:10.1134/S1607672916040104.
^ Zainullina LF, Ivanova TV, Sadovnikov SV, Vakhitova YV, Seredenin SB. Cognitive Enhancer Noopept Activates Transcription Factor HIF-1. Doklady. Biochemistry and Biophysics. 2020-09, 494 (1): 256–260. PMID 33119829. S2CID 226207175. doi:10.1134/S1607672920050129.
^ Vakhitova YV, Sadovnikov SV, Borisevich SS, Ostrovskaya RU, A Gudasheva T, Seredenin SB. Molecular Mechanism Underlying the Action of Substituted Pro-Gly Dipeptide Noopept. Acta Naturae. 2016, 8 (1): 82–89. PMC 4837574 . PMID 27099787. doi:10.32607/20758251-2016-8-1-82-89.
^ Lee SH, Golinska M, Griffiths JR. HIF-1-Independent Mechanisms Regulating Metabolic Adaptation in Hypoxic Cancer Cells 10 (9): 2371. 2021-09-09 [2025-05-15]. PMC 8472468 . PMID 34572020. doi:10.3390/cells10092371. （原始内容存档于2025-02-14）.
^ Tardner P. Finding the optimal dosage fornootropic agent Noopept: An analysis of available literature (PDF). International Journal of Environmental Science and Technology. 2020 [2025-05-15]. （原始内容存档 (PDF)于2025-02-20）.
^ Neznamov GG, Teleshova ES. Comparative studies of Noopept and piracetam in the treatment of patients with mild cognitive disorders in organic brain diseases of vascular and traumatic origin. Neuroscience and Behavioral Physiology. 2009-03, 39 (3): 311–321. PMID 19234797. S2CID 3348153. doi:10.1007/s11055-009-9128-4.

[2] 部分网站（页面存档备份，存于互联网档案馆）将Noopept翻译为诺普平，但并无官方来源依据。

[Examine-1] 1.0 ^1.1 ^1.2 ^1.3 Noopept Information. Examine.com. [2017-04-06].

[3] Proposed INN List 117. WHO Drug Information. 2017, 31 (2): 308 [2025-05-15]. （原始内容存档于2025-01-24）.

[4] Omberacetam. AdisInsight. Springer Nature Switzerland AG. [2018-05-12]. （原始内容存档于2017-10-15）（英语）. Alternative Names: DVD-111; GVS 111; Noopept

[Ostrovskaia_2002-5] 4.0 ^4.1 Ostrovskaia RU, Gudasheva TA, Voronina TA, Seredenin SB. [The original novel nootropic and neuroprotective agent noopept]. Eksperimental'naia i Klinicheskaia Farmakologiia. 2002, 65 (5): 66–72. PMID 12596521 （俄语）.

[6] Gudasheva TA, Boyko SS, Ostrovskaya RU, Voronina TA, Akparov VK, Trofimov SS, Rozantsev GG, Skoldinov AP, Zherdev VP, Seredenin SB. The major metabolite of dipeptide piracetam analogue GVS-111 in rat brain and its similarity to endogenous neuropeptide cyclo-L-prolylglycine. European Journal of Drug Metabolism and Pharmacokinetics. 1997, 22 (3): 245–252. PMID 9358206. doi:10.1007/BF03189814.

[7] Gudasheva TA, Koliasnikova KN, Alyaeva AG, Nikolaev SV, Antipova TA, Seredenin SB. Neuroprotective Effect of the Neuropeptide Cycloprolylglycine Depends on AMPA- and TrkB-Receptor Activation. Doklady. Biochemistry and Biophysics. 2022-12, 507 (1): 264–267. PMID 36786983. doi:10.1134/S1607672922060047.

[8] Gudasheva TA, Koliasnikova KN, Antipova TA, Seredenin SB. Neuropeptide cycloprolylglycine increases the levels of brain-derived neurotrophic factor in neuronal cells. Doklady. Biochemistry and Biophysics. 2016-07, 469 (1): 273–276. PMID 27599510. S2CID 254426990. doi:10.1134/S1607672916040104.

[9] Zainullina LF, Ivanova TV, Sadovnikov SV, Vakhitova YV, Seredenin SB. Cognitive Enhancer Noopept Activates Transcription Factor HIF-1. Doklady. Biochemistry and Biophysics. 2020-09, 494 (1): 256–260. PMID 33119829. S2CID 226207175. doi:10.1134/S1607672920050129.

[:0-10] Vakhitova YV, Sadovnikov SV, Borisevich SS, Ostrovskaya RU, A Gudasheva T, Seredenin SB. Molecular Mechanism Underlying the Action of Substituted Pro-Gly Dipeptide Noopept. Acta Naturae. 2016, 8 (1): 82–89. PMC 4837574 . PMID 27099787. doi:10.32607/20758251-2016-8-1-82-89.

[11] Lee SH, Golinska M, Griffiths JR. HIF-1-Independent Mechanisms Regulating Metabolic Adaptation in Hypoxic Cancer Cells 10 (9): 2371. 2021-09-09 [2025-05-15]. PMC 8472468 . PMID 34572020. doi:10.3390/cells10092371. （原始内容存档于2025-02-14）.

[12] Tardner P. Finding the optimal dosage fornootropic agent Noopept: An analysis of available literature (PDF). International Journal of Environmental Science and Technology. 2020 [2025-05-15]. （原始内容存档 (PDF)于2025-02-20）.

[13] Neznamov GG, Teleshova ES. Comparative studies of Noopept and piracetam in the treatment of patients with mild cognitive disorders in organic brain diseases of vascular and traumatic origin. Neuroscience and Behavioral Physiology. 2009-03, 39 (3): 311–321. PMID 19234797. S2CID 3348153. doi:10.1007/s11055-009-9128-4.

[1]

[注 1]

[2]

[3]

[4]

[5]

[6]

[7]

[8]

[9]

[10]

[11]

[12]