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本文引用的文献

1
(±)-Diinsininone: made nature's way.(±)-二异辛酮:源自天然。
Tetrahedron. 2006 May 29;62(22):5298-5307. doi: 10.1016/j.tet.2006.01.109.
2
Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor.高效且具选择性的基于苯吗喃的阿片δ受体反向激动剂。
J Med Chem. 2006 Sep 7;49(18):5597-609. doi: 10.1021/jm060459p.
3
N-substituted 4beta-methyl-5-(3-hydroxyphenyl)-7alpha-amidomorphans are potent, selective kappa opioid receptor antagonists.N-取代的4β-甲基-5-(3-羟基苯基)-7α-酰胺基吗啡喃是强效、选择性κ阿片受体拮抗剂。
J Med Chem. 2006 Mar 9;49(5):1781-91. doi: 10.1021/jm058264p.
4
Kappa opioid antagonists: past successes and future prospects.κ阿片受体拮抗剂:过去的成就与未来的前景
AAPS J. 2005 Oct 27;7(3):E704-22. doi: 10.1208/aapsj070371.
5
Effects of JDTic, a selective kappa-opioid receptor antagonist, on the development and expression of physical dependence on morphine using a rat continuous-infusion model.使用大鼠持续输注模型,研究选择性κ-阿片受体拮抗剂JDTic对吗啡身体依赖性形成和表达的影响。
Eur J Pharmacol. 2005 Nov 7;524(1-3):89-94. doi: 10.1016/j.ejphar.2005.09.013. Epub 2005 Oct 19.
6
Differential effects of the novel kappa opioid receptor antagonist, JDTic, on reinstatement of cocaine-seeking induced by footshock stressors vs cocaine primes and its antidepressant-like effects in rats.新型κ阿片受体拮抗剂JDTic对电击应激诱导的可卡因觅药行为恢复和可卡因激发诱导的可卡因觅药行为恢复的不同影响及其在大鼠中的抗抑郁样作用
Psychopharmacology (Berl). 2005 Nov;183(1):118-26. doi: 10.1007/s00213-005-0167-4. Epub 2005 Oct 22.
7
Pharmacological properties of JDTic: a novel kappa-opioid receptor antagonist.JDTic的药理学特性:一种新型κ-阿片受体拮抗剂。
Eur J Pharmacol. 2004 Oct 6;501(1-3):111-9. doi: 10.1016/j.ejphar.2004.08.028.
8
Inhibitory effect of the antidepressant St. John's wort (hypericum perforatum) on rat bladder contractility in vitro.抗抑郁药圣约翰草(贯叶连翘)对大鼠膀胱体外收缩力的抑制作用。
Urology. 2004 Jul;64(1):168-72. doi: 10.1016/j.urology.2004.02.021.
9
Study of the green tea polyphenols catechin-3-gallate (CG) and epicatechin-3-gallate (ECG) as proteasome inhibitors.绿茶多酚表没食子儿茶素没食子酸酯(CG)和表儿茶素没食子酸酯(ECG)作为蛋白酶体抑制剂的研究。
Bioorg Med Chem. 2004 Jul 1;12(13):3521-7. doi: 10.1016/j.bmc.2004.04.033.
10
Opioids and alcoholism.阿片类药物与酒精成瘾
Physiol Behav. 2004 Apr;81(2):339-58. doi: 10.1016/j.physbeh.2004.02.008.

黄酮类化合物作为阿片受体配体:鉴定及初步构效关系

Flavonoids as opioid receptor ligands: identification and preliminary structure-activity relationships.

作者信息

Katavic Peter L, Lamb Kenneth, Navarro Hernan, Prisinzano Thomas E

机构信息

Division of Medicinal & Natural Products Chemistry, College of Pharmacy, The University of Iowa, Iowa City, Iowa 52242, USA.

出版信息

J Nat Prod. 2007 Aug;70(8):1278-82. doi: 10.1021/np070194x. Epub 2007 Aug 9.

DOI:10.1021/np070194x
PMID:17685652
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2265593/
Abstract

Flavonoids have been recognized as the active ingredients of many medicinal plant extracts due to interactions with proteins via phenolic groups and low toxicity. Here, we report the investigation of the flavonoid core as a potential new scaffold for the development of opioid receptor ligands. Biological results suggest that stereochemistry of the C2 and C3 positions is important for antagonist activity and selectivity. Our results also suggest that the actions of Hypericum perforatum may be mediated in part by opioid receptors.

摘要

由于黄酮类化合物通过酚羟基与蛋白质相互作用且毒性较低,它们已被公认为许多药用植物提取物的活性成分。在此,我们报告了对黄酮类核心结构作为开发阿片受体配体潜在新支架的研究。生物学结果表明,C2和C3位的立体化学对拮抗剂活性和选择性很重要。我们的结果还表明,贯叶连翘的作用可能部分由阿片受体介导。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72e0/2265593/986cd701ba88/nihms41055f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72e0/2265593/71d6afb5aa8d/nihms41055f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72e0/2265593/4cb0fc17564b/nihms41055f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72e0/2265593/986cd701ba88/nihms41055f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72e0/2265593/71d6afb5aa8d/nihms41055f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72e0/2265593/4cb0fc17564b/nihms41055f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72e0/2265593/986cd701ba88/nihms41055f3.jpg