吡拉西坦, GluA1 的受体调节剂;GluA2 的受体调节剂;GluA3 的受体调节剂;GluA4 的受体调节剂

AMPA receptor Selective Inhibitors | Agonists | Antagonists | Modulators
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P408671-1ml
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Compound libraries (12332)

基本描述

英文别名 UCB 6215 | 1-Pyrrolidineacetamide, 2-oxo-
规格或纯度 Moligand™, 10mM in DMSO
英文名称 Piracetam
生化机理 吡拉西坦(UCB 6215)是神经递质γ-氨基丁酸(GABA)的环状衍生物,可用于治疗多种认知障碍。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 变构调节剂
作用机制 GluA1 的受体调节剂;GluA2 的受体调节剂;GluA3 的受体调节剂;GluA4 的受体调节剂
产品介绍

用途:

吡拉西坦用于研究6种吡拉西坦共晶体的晶体结构和理化性质。它还用于研究其体外抗氧化特性。

Information

Piracetam (UCB 6215) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.
In vitro

Piracetam is able to significantly decrease the fusogenic and destabilising effect of Abeta 29-42, in a concentration-dependent manner. Preincubation of piracetam, at a piracetam/peptide ratio of 960, during 20 min before the addition of Abeta 29-42 prevents almost completely the mixture of the two fluorescent probes. Preincubation of piracetam with lipids prevents almost completely the release of calcein induced by the peptide in a dose-dependent fashion (piracetam/peptide ratios from 9.6 to 960). Piracetam (< 1.0 mM) preincubated with brain membranes enhances membrane fluidity in aged mice, rats and humans, as indicated by decreased anisotropy of the membrane-bound fluorescence probe 1,6-diphenyl-1,3,5-hexatriene (DPH).

In vivo

Piracetam (300 mg/kg once daily) significantly increases membrane fluidity in some brain regions of young and aged rats, but has no measurable effect on membrane fluidity in the young rats. Piracetam (300 mg/kg daily for 6 weeks) improves active avoidance learning in the aged rats only and elevates membrane fluidity in all brain regions except the cerebellum in the aged rats. Piracetam (300 mg/kg daily for 6 weeks) also improves NMDA receptor density in the hippocampus and on muscarinic cholinergic receptor densities in the frontal cortex and the striatum and to a lesser extent in the hippocampus of rats. Piracetam (500 mg/kg p.o. for 14 days) elevates N-methyl-D-aspartate (NMDA) receptor density by about 20% and normalizes the enhanced affinity of L-glutamate for the NMDA receptor in aged mice. Piracetam-treated withdrawn rats has higher the number of synapses than that observed in nonpiracetam-treated and alcohol-fed animals by up to 20%, the mechanisms leading to the synaptic reorganization took place at the mossy fiber level.
Cell Data

cell lines:

Concentrations:

Incubation Time:

Powder Purity:≥100%

产品属性

ALogP -1.312
hba_count 2
HBD Count 1
Rotatable Bond 2

关联靶点(人)

GRIA4 Tclin 谷氨酸受体 4(Glutamate receptor 4) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
GRIA2 Tclin 谷氨酸受体 2(Glutamate receptor 2) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
GRIA3 Tclin 谷氨酸受体 3(Glutamate receptor 3) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
GRIA1 Tclin 谷氨酸受体 1(Glutamate receptor 1) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

Canonical SMILES NC(=O)CN1CCCC1=O
分子量 142.16

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 58 mg/mL (198.77 mM); Ethanol: 58 mg/mL (198.77 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility 72
DMSO(mM) Max Solubility 506.47
Water(mg / mL) Max Solubility 72
Water(mM) Max Solubility 506.47

安全和危险性(GHS)

技术规格说明书

Concentration(Compounding value) 9-11(mmol/L)
Record the entire process by video Conform

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

此产品的引用文献

1. Tingting Li, Like Lin, Cong Li, Jingyi Zheng, Bang Chen, Yehua Shen, Difeng Ren.  (2023)  Amelioration of walnut-derived novel peptides against D-galactose-induced cognitive impairment by modulating the gut microbiota composition.  Food & Function,  14  (9): (4228-4241).  [PMID:37067262] [10.1039/D2FO03775K]
2. Cui-Mei Liu, Hong-Yuan He, Lin Xu, Zhen-Dong Hua.  (2020)  New qualitative analysis strategy for illicit drugs using Raman spectroscopy and characteristic peaks method.  Drug Testing and Analysis,  13  (3): (720-728).  [PMID:33142047] [10.1002/dta.2963]
3. Xiaomeng Xu, Rong Liang, Dongmei Li, Chengyao Jiang, Songyi Lin.  (2020)  Evaluation of sea cucumber peptides-assisted memory activity and acetylation modification in hippocampus of test mice based on scopolamine-induced experimental animal model of memory disorder.  Journal of Functional Foods,  68  (103909).  [10.1016/j.jff.2020.103909]

参考文献

1. Tingting Li, Like Lin, Cong Li, Jingyi Zheng, Bang Chen, Yehua Shen, Difeng Ren.  (2023)  Amelioration of walnut-derived novel peptides against D-galactose-induced cognitive impairment by modulating the gut microbiota composition.  Food & Function,  14  (9): (4228-4241).  [PMID:37067262] [10.1039/D2FO03775K]
2. Cui-Mei Liu, Hong-Yuan He, Lin Xu, Zhen-Dong Hua.  (2020)  New qualitative analysis strategy for illicit drugs using Raman spectroscopy and characteristic peaks method.  Drug Testing and Analysis,  13  (3): (720-728).  [PMID:33142047] [10.1002/dta.2963]
3. Xiaomeng Xu, Rong Liang, Dongmei Li, Chengyao Jiang, Songyi Lin.  (2020)  Evaluation of sea cucumber peptides-assisted memory activity and acetylation modification in hippocampus of test mice based on scopolamine-induced experimental animal model of memory disorder.  Journal of Functional Foods,  68  (103909).  [10.1016/j.jff.2020.103909]

溶液计算器

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