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当前主题:脑渗透性神经降压素类似物

Current topics: brain penetrating neurotensin analog.

作者信息

Boules Mona, Fredrickson Paul, Richelson Elliott

机构信息

Neuropsychopharmacology Laboratory, Mayo Clinic, 4500 San Pablo Road, Jacksonville, FL 32224, USA.

出版信息

Life Sci. 2003 Oct 17;73(22):2785-92. doi: 10.1016/s0024-3205(03)00674-x.

DOI:10.1016/s0024-3205(03)00674-x
PMID:14511764
Abstract

Neurotensin (NT) is a neuropeptide found in the central nervous system and gastrointestinal tract. It is closely associated with dopaminergic and other neurotransmitter systems, and evidence supports a role for NT in various neuropsychiatric disorders. Because NT is readily degraded by peptidases, our group has developed various NT agonists that can be injected systemically, cross the blood brain barrier (BBB), yet retain the characteristics of native NT. The most widely studied and successful of these compounds, called NT69L, holds promise as a therapeutic agent for Parkinson's disease, schizophrenia, psychostimulant abuse and nicotine dependence, and serves as a tool to study the cellular and molecular effects of NT.

摘要

神经降压素(NT)是一种在中枢神经系统和胃肠道中发现的神经肽。它与多巴胺能及其他神经递质系统密切相关,有证据支持NT在各种神经精神疾病中发挥作用。由于NT很容易被肽酶降解,我们团队已开发出多种可全身注射、能穿过血脑屏障(BBB)且保留天然NT特性的NT激动剂。这些化合物中研究最广泛且最成功的一种,称为NT69L,有望成为治疗帕金森病、精神分裂症、精神兴奋剂滥用和尼古丁依赖的药物,并可作为研究NT细胞和分子效应的工具。

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1
Current topics: brain penetrating neurotensin analog.当前主题:脑渗透性神经降压素类似物
Life Sci. 2003 Oct 17;73(22):2785-92. doi: 10.1016/s0024-3205(03)00674-x.
2
Bioactive analogs of neurotensin: focus on CNS effects.神经降压素的生物活性类似物:聚焦于中枢神经系统效应
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Neurotensin agonists as an alternative to antipsychotics.神经降压素激动剂作为抗精神病药物的替代物。
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Effect of a novel neurotensin analog, NT69L, on nicotine-induced alterations in monoamine levels in rat brain.新型神经降压素类似物NT69L对尼古丁诱导的大鼠脑单胺水平变化的影响。
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Involvement of the neurotensin receptor 1 in the behavioral effects of two neurotensin agonists, NT-2 and NT69L: lack of hypothermic, antinociceptive and antipsychotic actions in receptor knockout mice.神经降压素受体1参与两种神经降压素激动剂NT-2和NT69L的行为效应:受体基因敲除小鼠缺乏体温降低、抗伤害感受和抗精神病作用。
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Brain Res. 2003 Jul 25;979(1-2):245-8. doi: 10.1016/s0006-8993(03)02895-6.
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A neurotensin analog, NT69L, attenuates intravenous nicotine self-administration in rats.一种神经降压素类似物 NT69L 可减弱大鼠静脉注射尼古丁的自我给药。
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Effects of a novel neurotensin peptide analog given extracranially on CNS behaviors mediated by apomorphine and haloperidol.颅外给予一种新型神经降压素肽类似物对由阿扑吗啡和氟哌啶醇介导的中枢神经系统行为的影响。
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Selective tolerance to the hypothermic and anticataleptic effects of a neurotensin analog that crosses the blood-brain barrier.对一种能穿越血脑屏障的神经降压素类似物的低温和抗僵住效应的选择性耐受。
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Diverse roles of neurotensin agonists in the central nervous system.神经降压素激动剂在中枢神经系统中的多种作用。
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NTS-Polyplex: a potential nanocarrier for neurotrophic therapy of Parkinson's disease.NTS-聚集体:一种用于帕金森病神经保护治疗的潜在纳米载体。
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The role of NTS2 in the development of tolerance to NT69L in mouse models for hypothermia and thermal analgesia.NTS2 在低温和热镇痛小鼠模型中对 NT69L 耐受发展的作用。
Behav Brain Res. 2011 Oct 31;224(2):344-9. doi: 10.1016/j.bbr.2011.06.014. Epub 2011 Jun 21.
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Similarities in the behavior and molecular deficits in the frontal cortex between the neurotensin receptor subtype 1 knockout mice and chronic phencyclidine-treated mice: relevance to schizophrenia.神经降压素受体亚型 1 敲除小鼠和慢性苯环己哌啶处理小鼠前额皮质行为和分子缺陷的相似性:与精神分裂症的相关性。
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Chronic NT69L potently prevents drug-induced disruption of prepulse inhibition without causing tolerance.慢性 NT69L 有力地预防了药物引起的前脉冲抑制中断,而不会导致耐受。
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