• 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

关于阿片类药物和脑啡肽生物活性构象的提议。

Proposal for the biologically active conformation of opiates and enkephalin.

作者信息

Gorin F A, Marshall G R

出版信息

Proc Natl Acad Sci U S A. 1977 Nov;74(11):5179-83. doi: 10.1073/pnas.74.11.5179.

DOI:10.1073/pnas.74.11.5179
PMID:270758
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC432125/
Abstract

A model for the opiate receptor has been defined by using a computer-based molecular display and x-ray crystallographic input data. The model can explain the stereochemical fashion in which the morphine, morphinan, and oripavine classes of compounds interact with the receptor. The minimal structural unit of the enkephalins demonstrated to be pharmacologically active. Tyr-Gly-Gly-Phe, was also fitted to this model by using a systematic search of conformational space.

摘要

通过使用基于计算机的分子展示和X射线晶体学输入数据，已经定义了一种阿片受体模型。该模型可以解释吗啡、吗啡喃和阿扑吗啡类化合物与受体相互作用的立体化学方式。已证明具有药理活性的脑啡肽的最小结构单元Tyr-Gly-Gly-Phe，也通过对构象空间的系统搜索拟合到该模型中。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9725/432125/546f34602653/pnas00033-0481-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9725/432125/546f34602653/pnas00033-0481-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9725/432125/546f34602653/pnas00033-0481-a.jpg

相似文献

1
Proposal for the biologically active conformation of opiates and enkephalin.关于阿片类药物和脑啡肽生物活性构象的提议。
Proc Natl Acad Sci U S A. 1977 Nov;74(11):5179-83. doi: 10.1073/pnas.74.11.5179.
2
Structure-activity studies of narcotic agonists and antagonists from quantum chemical calculations.基于量子化学计算的麻醉性激动剂和拮抗剂的构效关系研究
NIDA Res Monogr. 1978(22):278-316.
3
Stereochemical considerations in structural comparison of enkephalins and endorphins with exogenous opiate agents.脑啡肽和内啡肽与外源性阿片制剂结构比较中的立体化学考量
J Pharm Sci. 1978 Apr;67(4):590-1. doi: 10.1002/jps.2600670448.
4
Conformation of [Leu5]enkephalin from X-ray diffraction: features important for recognition at opiate receptor.通过X射线衍射确定的[亮氨酸5]脑啡肽的构象：对阿片受体识别重要的特征
Science. 1978 Mar 17;199(4334):1214-6. doi: 10.1126/science.204006.
5
The enkephalins and opiates: structure-activity relations.脑啡肽与阿片类药物：构效关系
J Pharm Pharmacol. 1977 May;29(5):257-65. doi: 10.1111/j.2042-7158.1977.tb11308.x.
6
X-ray diffraction studies of enkephalins and opiates.
NIDA Res Monogr. 1988;87:41-59.
7
Elucidation of the receptor-bound conformation of the enkephalins.
J Supramol Struct. 1978;9(1):27-39. doi: 10.1002/jss.400090104.
8
Affinities of opiate agonists and antagonists for the enkephalin receptors of rat brain.阿片类激动剂和拮抗剂对大鼠脑内脑啡肽受体的亲和力。
Res Commun Chem Pathol Pharmacol. 1977 Apr;16(4):749-52.
9
Modulation of dopamine release in rat striatal slices by delta opiate agonists.δ阿片受体激动剂对大鼠纹状体切片中多巴胺释放的调节作用。
J Pharmacol Exp Ther. 1982 Aug;222(2):435-40.
10
A cyclic enkephalin analog with high in vitro opiate activity.一种具有高体外阿片样活性的环脑啡肽类似物。
Proc Natl Acad Sci U S A. 1980 Dec;77(12):7162-6. doi: 10.1073/pnas.77.12.7162.

引用本文的文献

1
Applications of biaryl cyclization in the synthesis of cyclic enkephalin analogs with a highly restricted flexibility.联芳环化在合成具有高度受限柔韧性的环状脑啡肽类似物中的应用。
Amino Acids. 2024 Mar 1;56(1):18. doi: 10.1007/s00726-023-03371-5.
2
A DFT and semiempirical model-based study of opioid receptor affinity and selectivity in a group of molecules with a morphine structural core.基于密度泛函理论（DFT）和半经验模型对一组具有吗啡结构核心的分子中阿片受体亲和力和选择性的研究。
Int J Med Chem. 2012;2012:682495. doi: 10.1155/2012/682495. Epub 2012 Dec 13.
3
Consensus 3D model of μ-opioid receptor ligand efficacy based on a quantitative Conformationally Sampled Pharmacophore.

本文引用的文献

1
The crystal and molecular stucture of 7-alpha-(1-(r)-hydroxy-1-methylbutyl)-6,14-endo-ethenotetrahydrothebaine hydrobromide (19 -propylthevinol hydrobromide).
J Am Chem Soc. 1967 Jun 7;89(12):2901-5. doi: 10.1021/ja00988a017.
2
A new concept on the mode of interaction of narcotic analgesics with receptors.
J Med Chem. 1965 Sep;8(5):609-16. doi: 10.1021/jm00329a013.
3
Narcotic analgesics and antagonists.麻醉性镇痛药及拮抗剂。
Annu Rev Pharmacol. 1971;11:241-70. doi: 10.1146/annurev.pa.11.040171.001325.
4
基于定量构象采样药效团的 μ 阿片受体配体效力共识 3D 模型。
J Phys Chem B. 2011 Jun 9;115(22):7487-96. doi: 10.1021/jp202542g. Epub 2011 May 12.
4
Influence of intramolecular hydrogen bonding on the electronic structure of oxymorphone.分子内氢键对羟吗啡酮电子结构的影响。
Proc Natl Acad Sci U S A. 1980 Oct;77(10):5602-5. doi: 10.1073/pnas.77.10.5602.
5
Development of a common 3D pharmacophore for delta-opioid recognition from peptides and non-peptides using a novel computer program.使用一种新型计算机程序开发用于从肽和非肽中识别δ-阿片受体的通用三维药效团。
J Comput Aided Mol Des. 1997 Jan;11(1):21-8. doi: 10.1023/a:1008067209563.
6
Comparison of cyclic delta-opioid peptides with non-peptide delta-agonist spiroindanyloxymorphone (SIOM) using the message-address concept: a molecular modeling study.使用信息-靶点概念比较环化δ-阿片肽与非肽δ-激动剂螺茚满氧基吗啡（SIOM）：一项分子建模研究。
J Comput Aided Mol Des. 1996 Aug;10(4):327-36. doi: 10.1007/BF00124502.
7
Frog skin opioid peptides: a case for environmental mimicry.蛙皮阿片肽：环境模拟的一个实例
Environ Health Perspect. 1994 Aug;102(8):648-54. doi: 10.1289/ehp.94102648.
8
To the problem of biologically active conformation of enkephalin.针对脑啡肽生物活性构象的问题。
Mol Cell Biochem. 1981 Jan 20;34(1):23-9. doi: 10.1007/BF02354848.
9
X-ray diffraction studies of enkephalins. Crystal structure of [(4'-bromo) Phe4,Leu5]enkephalin.脑啡肽的X射线衍射研究。[(4'-溴)苯丙氨酸4，亮氨酸5]脑啡肽的晶体结构。
Biochem J. 1984 Mar 15;218(3):677-89. doi: 10.1042/bj2180677.
10
A cyclic enkephalin analog with high in vitro opiate activity.一种具有高体外阿片样活性的环脑啡肽类似物。
Proc Natl Acad Sci U S A. 1980 Dec;77(12):7162-6. doi: 10.1073/pnas.77.12.7162.
Importance of the nitrogen lone electron pair orientation in stereospecific opiates.立体特异性阿片中氮孤对电子取向的重要性。
J Med Chem. 1974 Aug;17(8):907-8. doi: 10.1021/jm00254a029.
5
A new example of a morphine-sensitive neuro-effector junction: adrenergic transmission in the mouse vas deferens.吗啡敏感型神经效应器连接的一个新实例：小鼠输精管中的肾上腺素能传递。
Br J Pharmacol. 1972 Dec;46(4):764-6. doi: 10.1111/j.1476-5381.1972.tb06901.x.
6
Methadone.美沙酮
Can Med Assoc J. 1973 Oct 6;109(7):615-9.
7
A neuroblastoma times glioma hybrid cell line with morphine receptors.一种具有吗啡受体的神经母细胞瘤-胶质瘤杂交细胞系。
Proc Natl Acad Sci U S A. 1974 Sep;71(9):3474-7. doi: 10.1073/pnas.71.9.3474.
8
Pharmacological implications of the conformation of the methadone base.美沙酮碱构象的药理学意义
Nat New Biol. 1973 Aug 8;244(136):186-7. doi: 10.1038/newbio244186b0.
9
Structural and conformational relationships between the enkephalins and the opiates.脑啡肽与阿片类药物之间的结构和构象关系。
Nature. 1976 Apr 29;260(5554):795-7. doi: 10.1038/260795a0.
10
Biosynthetic origin and receptor conformation of methionine enkephalin.甲硫氨酸脑啡肽的生物合成起源与受体构象
Nature. 1976 Mar 11;260(5547):165-6. doi: 10.1038/260165a0.