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本文引用的文献

1
Univalent and bivalent ligands of butorphan: characteristics of the linking chain determine the affinity and potency of such opioid ligands.布托啡诺的单价和二价配体：连接链的特性决定了此类阿片样物质配体的亲和力和效价。
J Med Chem. 2009 Dec 10;52(23):7389-96. doi: 10.1021/jm900379p.
2
Synthesis and pharmacological evaluation of hydrophobic esters and ethers of butorphanol at opioid receptors.布托啡诺的疏水酯类和醚类在阿片受体处的合成及药理学评价
Bioorg Med Chem Lett. 2008 Aug 15;18(16):4474-6. doi: 10.1016/j.bmcl.2008.07.054. Epub 2008 Jul 17.
3
In vivo characterization of (-)(-)MCL-144 and (+)(-)MCL-193: isomeric, bivalent ligands with mu/kappa agonist properties.(-)(-)MCL-144和(+)(-)MCL-193的体内特性：具有μ/κ激动剂特性的同分异构二价配体。
Neurochem Res. 2008 Oct;33(10):2142-50. doi: 10.1007/s11064-008-9752-3. Epub 2008 Jun 5.
4
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 4. Opioid receptor binding properties of 8-[N-(4'-phenyl)-phenethyl)carboxamido] analogues of cyclazocine and ethylketocycalzocine.重新定义2,6-亚甲基-3-苯并氮杂䓬的构效关系。4. 环唑辛和乙基酮环唑辛的8-[N-(4'-苯基)-苯乙基]甲酰胺类似物的阿片受体结合特性。
J Med Chem. 2006 Sep 7;49(18):5635-9. doi: 10.1021/jm060278n.
5
Characterization of a novel bivalent morphinan possessing kappa agonist and micro agonist/antagonist properties.一种具有κ激动剂和微激动剂/拮抗剂特性的新型二价吗啡喃的表征。
J Pharmacol Exp Ther. 2005 Nov;315(2):821-7. doi: 10.1124/jpet.105.084343. Epub 2005 Aug 2.
6
A heterodimer-selective agonist shows in vivo relevance of G protein-coupled receptor dimers.一种异二聚体选择性激动剂显示了G蛋白偶联受体二聚体在体内的相关性。
Proc Natl Acad Sci U S A. 2005 Jun 21;102(25):9050-5. doi: 10.1073/pnas.0501112102. Epub 2005 Jun 2.
7
A role for heterodimerization of mu and delta opiate receptors in enhancing morphine analgesia.μ和δ阿片受体异源二聚化在增强吗啡镇痛作用中的作用。
Proc Natl Acad Sci U S A. 2004 Apr 6;101(14):5135-9. doi: 10.1073/pnas.0307601101. Epub 2004 Mar 24.
8
Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.新型二聚体吗啡喃类κ和μ阿片受体配体的设计与合成
J Med Chem. 2003 Nov 20;46(24):5162-70. doi: 10.1021/jm030139v.
9
Identity of the putative delta1-opioid receptor as a delta-kappa heteromer in the mouse spinal cord.假定的δ1阿片受体在小鼠脊髓中作为δ-κ异聚体的身份。
Eur J Pharmacol. 2003 Apr 25;467(1-3):233-4. doi: 10.1016/s0014-2999(03)01599-1.
10
Effects of mixed-action kappa/mu opioids on cocaine self-administration and cocaine discrimination by rhesus monkeys.混合作用的κ/μ阿片类药物对恒河猴可卡因自我给药及可卡因辨别能力的影响。
Neuropsychopharmacology. 2003 Jun;28(6):1125-39. doi: 10.1038/sj.npp.1300105. Epub 2003 Mar 5.

连接子取代对丁丙诺啡单价和双价配体与阿片受体结合的影响。

Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors.

机构信息

Alcohol and Drug Abuse Research Center, McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA.

出版信息

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1507-9. doi: 10.1016/j.bmcl.2010.01.101. Epub 2010 Jan 25.

DOI:10.1016/j.bmcl.2010.01.101
PMID:20144870
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2834170/
Abstract

A series of bivalent hydroxy ether butorphan ligands were prepared and their binding affinities at the opioid receptors determined. Addition of a hydroxy group to a hydrocarbon chain can potentiate binding affinity up to 27- and 86-fold at the mu and kappa opioid receptors, respectively. Two bivalent ligands with sub-nanomolar binding affinity at the mu and kappa opioid receptors were discovered.

摘要

制备了一系列二价羟乙醚丁丙诺啡配体，并测定了它们在阿片受体上的结合亲和力。在烃链上添加一个羟基可以使μ和κ阿片受体的结合亲和力分别增强 27 倍和 86 倍。发现了两种具有亚纳摩尔结合亲和力的二价配体，分别在μ和κ阿片受体上。