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Bioactivity Of Neuropeptides

Bioactivity Of Neuropeptides
神经肽的生物活性
批准号：
6673283
负责人：
LAWRENCE H LAZARUS
金额：
$0.0万
依托单位：
NATIONAL INSTITUTE OF ENVIRONMENTAL HEALTH SCIENCES
依托单位国家：
美国
项目类别：
财政年份：
--
资助国家：
美国
项目状态：
未结题
起止时间：
至
来源：
https://reporter.nih.gov/project-details/6673283
关键词：
endogenous opioid neuropeptides peptide analog pharmacokinetics

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中文摘要
翻译
工作概述：研究了新开发的阿片类似物在小鼠体内的药理和生理活性。生物活性谱与体外药理学数据相似，反映了受体结合亲和力（详见以前的项目）。一些具有激动作用的合成类似物比对照物质弱（对δ受体的δ torphin或对μ受体的吗啡）；然而，使用标准测试程序，一些药物在产生镇痛作用方面明显优于吗啡（2- 25倍）。事实上，这些化合物正在日本申请专利，此时披露将危及这一进程。
英文摘要
Summary of Work: The pharmacological and physiological activity of recently developed opioid analogues were determined in mice. The bioactivity profile paralled that of the in vitro pharmacological data and reflected the receptor binding affinity (see previous projects for details). Some synthetic analogues which exhibited agonism were weaker than the control substances (deltorphin for delta or morphine for mu receptors); however, some were substantially better (2- to 25-fold) than morphine in generating analgesia using standard testing procedures. In fact, these compounds are under patent application in Japan and disclosure at this time would jepardize that process.
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MOLECULAR DYNAMICS CONFORMATION OF OPIOID PEPTIDES
MOLECULAR DYNAMICS CONFORMATION OF OPIOID PEPTIDES
Bioactivity Of Neuropeptides
Molecular Dynamics Conformation Of Opioid Peptides
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