• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

相似文献

1
PAOPA, a potent analogue of Pro-Leu-glycinamide and allosteric modulator of the dopamine D2 receptor, prevents NMDA receptor antagonist (MK-801)-induced deficits in social interaction in the rat: implications for the treatment of negative symptoms in schizophrenia.PAOPA，一种强效 Pro-Leu-甘氨酰胺类似物和多巴胺 D2 受体变构调节剂，可预防 NMDA 受体拮抗剂（MK-801）引起的大鼠社交互动缺陷：对精神分裂症阴性症状治疗的意义。
Schizophr Res. 2011 Jan;125(1):88-92. doi: 10.1016/j.schres.2010.09.025. Epub 2010 Oct 30.
2
The Effect of PAOPA, a Novel Allosteric Modulator of Dopamine D2 Receptors, on Signaling Proteins Following Sub-Chronic Administration in Rats.新型多巴胺 D2 受体变构调节剂 PAOPA 对大鼠亚慢性给药后信号蛋白的影响。
Curr Mol Pharmacol. 2021 Oct 25;14(4):469-476. doi: 10.2174/1874467213666200910091007.
3
Modulation of high-affinity CNS dopamine D2 receptor by L-pro-L-leu-glycinamide (PLG) analogue 3(R)-(N-L-prolylamino)-2-oxo-1-pyrrolidineacetamide.L-脯氨酰-L-亮氨酰-甘氨酰胺（PLG）类似物3(R)-(N-脯氨酰胺基)-2-氧代-1-吡咯烷乙酰胺对中枢神经系统高亲和力多巴胺D2受体的调节作用
Prog Neuropsychopharmacol Biol Psychiatry. 1990;14(5):821-7. doi: 10.1016/0278-5846(90)90054-k.
4
Modulation of dopamine receptor agonist-induced rotational behavior in 6-OHDA-lesioned rats by a peptidomimetic analogue of Pro-Leu-Gly-NH2 (PLG).脯氨酸-亮氨酸-甘氨酸-酰胺（PLG）的拟肽类似物对6-羟基多巴胺损伤大鼠中多巴胺受体激动剂诱导的旋转行为的调节作用
Peptides. 1997;18(8):1209-15. doi: 10.1016/s0196-9781(97)00147-2.
5
L-prolyl-l-leucyl-glycinamide and its peptidomimetic analog 3(R)-[(2(S)-pyrrolidylcarbonyl)amino]-2-oxo-1-pyrrolidineacetamide (PAOPA) attenuate haloperidol-induced c-fos expression in the striatum.L-脯氨酰-L-亮氨酰-甘氨酰胺及其拟肽类似物3(R)-[(2(S)-吡咯烷基羰基)氨基]-2-氧代-1-吡咯烷乙酰胺（PAOPA）可减弱氟哌啶醇诱导的纹状体中c-fos的表达。
Peptides. 2000 Feb;21(2):301-8. doi: 10.1016/s0196-9781(99)00194-1.
6
Pro-Leu-glycinamide and its peptidomimetic, PAOPA, attenuate haloperidol induced vacuous chewing movements in rat: A model of human tardive dyskinesia.脯氨酸-亮氨酸-甘氨酰胺及其拟肽PAOPA可减轻氟哌啶醇诱导的大鼠空嚼运动：一种人类迟发性运动障碍模型。
Peptides. 2003 Feb;24(2):313-9. doi: 10.1016/s0196-9781(03)00045-7.
7
Modulation of agonist stimulated adenylyl cyclase and GTPase activity by L-pro-L-leu-glycinamide and its peptidomimetic analogue in rat striatal membranes.L-脯氨酰-L-亮氨酰-甘氨酰胺及其拟肽类似物对大鼠纹状体膜中激动剂刺激的腺苷酸环化酶和GTP酶活性的调节作用。
Neurosci Lett. 1999 Jul 2;269(1):21-4. doi: 10.1016/s0304-3940(99)00413-9.
8
PAOPA, a potent dopamine D2 receptor allosteric modulator, prevents and reverses behavioral and biochemical abnormalities in an amphetamine-sensitized preclinical animal model of schizophrenia.PAOPA，一种有效的多巴胺 D2 受体变构调节剂，可预防和逆转精神分裂症的安非他命敏化临床前动物模型中的行为和生化异常。
Eur Neuropsychopharmacol. 2013 Mar;23(3):253-62. doi: 10.1016/j.euroneuro.2012.04.010. Epub 2012 May 30.
9
Effects of the dopamine D2 allosteric modulator, PAOPA, on the expression of GRK2, arrestin-3, ERK1/2, and on receptor internalization.PAOPA 对多巴胺 D2 变构调节剂、GRK2、arrestin-3、ERK1/2 的表达及受体内化的影响。
PLoS One. 2013 Aug 6;8(8):e70736. doi: 10.1371/journal.pone.0070736. Print 2013.
10
Protection against MPTP treatment by an analog of Pro-Leu-Gly-NH2 (PLG, MIF-1).Pro-Leu-Gly-NH2（PLG，MIF-1）类似物对MPTP治疗的保护作用。
Peptides. 1998;19(2):403-6. doi: 10.1016/s0196-9781(97)00321-5.

引用本文的文献

1
Review on allosteric modulators of dopamine receptors so far.多巴胺受体变构调节剂的研究综述（截至目前）
Health Sci Rep. 2024 Mar 18;7(3):e1984. doi: 10.1002/hsr2.1984. eCollection 2024 Mar.
2
Allosteric Modulators of Dopamine D Receptors for Fine-Tuning of Dopaminergic Neurotransmission in CNS Diseases: Overview, Pharmacology, Structural Aspects and Synthesis.中枢神经系统疾病中多巴胺 D 受体的变构调节剂：概述、药理学、结构方面和合成。
Molecules. 2022 Dec 25;28(1):178. doi: 10.3390/molecules28010178.
3
Allosteric Modulator Leads Hiding in Plain Site: Developing Peptide and Peptidomimetics as GPCR Allosteric Modulators.隐匿于显而易见之处的变构调节剂先导物：开发肽类和拟肽类作为G蛋白偶联受体变构调节剂
Front Chem. 2021 Oct 7;9:671483. doi: 10.3389/fchem.2021.671483. eCollection 2021.
4
Molecular Basis of GABA Hypofunction in Adolescent Schizophrenia-Like Animals.青少年精神分裂症样动物 GABA 功能低下的分子基础。
Neural Plast. 2021 Apr 15;2021:9983438. doi: 10.1155/2021/9983438. eCollection 2021.
5
1MeTIQ and olanzapine, despite their neurochemical impact, did not ameliorate performance in fear conditioning and social interaction tests in an MK-801 rat model of schizophrenia.1 美替拉酮和奥氮平，尽管对神经化学有影响，但未能改善 MK-801 致精神分裂症大鼠模型的恐惧条件反射和社会互动测试中的表现。
Pharmacol Rep. 2021 Apr;73(2):490-505. doi: 10.1007/s43440-020-00209-9. Epub 2021 Jan 6.
6
Allosteric Modulators of G Protein-Coupled Dopamine and Serotonin Receptors: A New Class of Atypical Antipsychotics.G蛋白偶联多巴胺和5-羟色胺受体的变构调节剂：一类新型非典型抗精神病药物。
Pharmaceuticals (Basel). 2020 Nov 14;13(11):388. doi: 10.3390/ph13110388.
7
The Dopamine Allosteric Agent, PAOPA, Demonstrates Therapeutic Potential in the Phencyclidine NMDA Pre-clinical Rat Model of Schizophrenia.多巴胺变构剂PAOPA在苯环利定NMDA精神分裂症临床前大鼠模型中显示出治疗潜力。
Front Behav Neurosci. 2018 Dec 12;12:302. doi: 10.3389/fnbeh.2018.00302. eCollection 2018.
8
Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts.变构调节 A 类 G 蛋白偶联受体：靶点、药物及新的概念。
J Med Chem. 2019 Jan 10;62(1):88-127. doi: 10.1021/acs.jmedchem.8b00875. Epub 2018 Aug 28.
9
Permeation of Polymethoxyflavones into the Mouse Brain and Their Effect on MK-801-Induced Locomotive Hyperactivity.聚甲氧基黄酮向小鼠脑内的渗透及其对MK-801诱导的运动性多动的影响。
Int J Mol Sci. 2017 Feb 24;18(3):489. doi: 10.3390/ijms18030489.
10
Effects of the dopamine D2 allosteric modulator, PAOPA, on the expression of GRK2, arrestin-3, ERK1/2, and on receptor internalization.PAOPA 对多巴胺 D2 变构调节剂、GRK2、arrestin-3、ERK1/2 的表达及受体内化的影响。
PLoS One. 2013 Aug 6;8(8):e70736. doi: 10.1371/journal.pone.0070736. Print 2013.

本文引用的文献

1
Impact of D2 receptor internalization on binding affinity of neuroimaging radiotracers.D2 受体内化对神经影像学示踪剂结合亲和力的影响。
Neuropsychopharmacology. 2010 Feb;35(3):806-17. doi: 10.1038/npp.2009.189. Epub 2009 Dec 2.
2
G protein-coupled receptor kinase-mediated phosphorylation regulates post-endocytic trafficking of the D2 dopamine receptor.G蛋白偶联受体激酶介导的磷酸化作用调节D2多巴胺受体的内吞后转运。
J Biol Chem. 2009 May 29;284(22):15038-51. doi: 10.1074/jbc.M900388200. Epub 2009 Mar 30.
3
Allosteric modulation of the dopamine D2 receptor by Pro-Leu-Gly-NH2 peptidomimetics constrained in either a polyproline II helix or a type II beta-turn conformation.在聚脯氨酸II螺旋或II型β-转角构象中受到限制的Pro-Leu-Gly-NH2拟肽对多巴胺D2受体的变构调节。
J Med Chem. 2009 Apr 9;52(7):2043-51. doi: 10.1021/jm801575w.
4
Pharmacological characterization of 2-methoxy-N-propylnorapomorphine's interactions with D2 and D3 dopamine receptors.2-甲氧基-N-丙基去甲阿扑吗啡与D2和D3多巴胺受体相互作用的药理学特征
Synapse. 2009 Jun;63(6):462-75. doi: 10.1002/syn.20626.
5
Circuit-based framework for understanding neurotransmitter and risk gene interactions in schizophrenia.基于回路的框架，用于理解精神分裂症中的神经递质与风险基因相互作用。
Trends Neurosci. 2008 May;31(5):234-42. doi: 10.1016/j.tins.2008.02.005. Epub 2008 Apr 7.
6
A single application of MK801 causes symptoms of acute psychosis, deficits in spatial memory, and impairment of synaptic plasticity in rats.单次应用MK801会导致大鼠出现急性精神病症状、空间记忆缺陷以及突触可塑性受损。
Hippocampus. 2008;18(2):125-34. doi: 10.1002/hipo.20367.
7
MIF-1 and its peptidomimetic analogs attenuate haloperidol-induced vacuous chewing movements and modulate apomorphine-induced rotational behavior in 6-hydroxydopamine-lesioned rats.巨噬细胞移动抑制因子-1（MIF-1）及其拟肽类似物可减轻氟哌啶醇诱导的6-羟基多巴胺损伤大鼠的空嚼运动，并调节阿扑吗啡诱导的旋转行为。
Peptides. 2007 Oct;28(10):2009-15. doi: 10.1016/j.peptides.2007.07.026. Epub 2007 Aug 1.
8
Modulation of agonist binding to human dopamine receptor subtypes by L-prolyl-L-leucyl-glycinamide and a peptidomimetic analog.L-脯氨酰-L-亮氨酰-甘氨酰胺及一种拟肽类似物对激动剂与人多巴胺受体亚型结合的调节作用。
J Pharmacol Exp Ther. 2005 Dec;315(3):1228-36. doi: 10.1124/jpet.105.091256. Epub 2005 Aug 26.
9
(+)-MK-801 induced social withdrawal in rats; a model for negative symptoms of schizophrenia.（+）-MK-801诱导大鼠出现社交退缩；一种精神分裂症阴性症状的模型。
Prog Neuropsychopharmacol Biol Psychiatry. 2005 Jun;29(5):827-32. doi: 10.1016/j.pnpbp.2005.03.004.
10
Transient N-methyl-D-aspartate receptor blockade in early development causes lasting cognitive deficits relevant to schizophrenia.早期发育过程中短暂的N-甲基-D-天冬氨酸受体阻断会导致与精神分裂症相关的持久性认知缺陷。
Biol Psychiatry. 2005 Feb 15;57(4):433-6. doi: 10.1016/j.biopsych.2004.11.031.

PAOPA，一种强效 Pro-Leu-甘氨酰胺类似物和多巴胺 D2 受体变构调节剂，可预防 NMDA 受体拮抗剂（MK-801）引起的大鼠社交互动缺陷：对精神分裂症阴性症状治疗的意义。

PAOPA, a potent analogue of Pro-Leu-glycinamide and allosteric modulator of the dopamine D2 receptor, prevents NMDA receptor antagonist (MK-801)-induced deficits in social interaction in the rat: implications for the treatment of negative symptoms in schizophrenia.

机构信息

Department of Psychiatry and Behavioural Neurosciences, McMaster University, Hamilton, ON, Canada.

出版信息

Schizophr Res. 2011 Jan;125(1):88-92. doi: 10.1016/j.schres.2010.09.025. Epub 2010 Oct 30.

DOI:10.1016/j.schres.2010.09.025
PMID:21036015
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3010311/
Abstract

The aim of this study was to investigate whether a potent analogue of the endogenous brain peptide l-prolyl-l-leucyl-glycinamide (PLG), (3(R)-[(2(S)-pyrrolidinylcarbonyl)amino]-2-oxo-1-pyrrolidineacetamide (PAOPA), can prevent the induction of social withdrawal caused by sub-chronic treatment with the non-competitive NMDA (N-methyl-l-aspartate) receptor antagonist, MK-801. Results indicate that MK-801 (0.5 mg/kg) significantly decreased social interaction following sub-chronic treatment (7 days). Treatment with PAOPA (1 mg/kg) blocked the effects of MK-801, and increased the amount of time spent in social interaction in comparison to control animals. These results provide evidence for the development of peptidomimetic compounds for the treatment of social withdrawal and related negative symptoms associated with schizophrenia.

摘要

这项研究的目的是探讨内源性脑肽 l-脯氨酰-l-亮氨酰-甘氨酰胺的一种有效类似物（PLG）（3(R)-[(2(S)-吡咯烷羰基)氨基]-2-氧代-1-吡咯烷乙酰胺（PAOPA））是否可以预防亚慢性给予非竞争性 NMDA（N-甲基-D-天冬氨酸）受体拮抗剂 MK-801 引起的社交回避的诱导。结果表明，MK-801（0.5mg/kg）在亚慢性治疗（7 天）后显著减少社交互动。PAOPA（1mg/kg）治疗阻断了 MK-801 的作用，并与对照动物相比，增加了社交互动的时间。这些结果为开发用于治疗社交回避和与精神分裂症相关的阴性症状的肽模拟化合物提供了证据。