羟吗啡吲哚的5'-卤代类似物。
5'-halogenated analogs of oxymorphindole.
作者信息
Metcalf Matthew D, Coop Andrew
机构信息
Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 Penn Street, Baltimore, MD 21201, USA.
出版信息
Bioorg Med Chem Lett. 2007 Nov 1;17(21):5916-7. doi: 10.1016/j.bmcl.2007.07.098. Epub 2007 Aug 23.
Abstract
The presence of a 6,7-fused indole group in the indolomorphinans was considered to be responsible for the delta opioid selectivity for this class of ligands. Herein is shown that 5'-halogenated analogs of oxymorphindole are opioids with little selectivity for delta receptors over mu opioid receptors.
摘要
吲哚omorphinans中6,7-稠合吲哚基团的存在被认为是这类配体对δ阿片受体具有选择性的原因。本文表明，羟吗啡酮的5'-卤代类似物是对δ受体与μ阿片受体选择性较低的阿片类药物。
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本文引用的文献
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Role of delivery and trafficking of delta-opioid peptide receptors in opioid analgesia and tolerance.δ-阿片肽受体的转运与运输在阿片类镇痛及耐受性中的作用
Trends Pharmacol Sci. 2006 Jun;27(6):324-9. doi: 10.1016/j.tips.2006.04.005. Epub 2006 May 6.
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Opioid ligands with mixed mu/delta opioid receptor interactions: an emerging approach to novel analgesics.具有μ/δ阿片受体混合相互作用的阿片类配体：新型镇痛药的一种新兴方法。
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N-Cyclohexylethyl-N-noroxymorphindole: a mu-opioid preferring analogue of naltrindole.N-环己基乙基-N-去甲羟吗啡吲哚：一种对μ阿片受体具有选择性的纳曲吲哚类似物。
Bioorg Med Chem Lett. 2000 Nov 6;10(21):2449-51. doi: 10.1016/s0960-894x(00)00479-0.
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Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.纳曲酮衍生的吡啶并和嘧啶并吗啡喃的合成、阿片受体结合及生物活性
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The opioid mu agonist/delta antagonist DIPP-NH(2)[Psi] produces a potent analgesic effect, no physical dependence, and less tolerance than morphine in rats.阿片类μ激动剂/δ拮抗剂DIPP-NH(2)[Psi]在大鼠中产生强效镇痛作用，无身体依赖性，且耐受性比吗啡小。
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delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole.与纳曲吲哚相关的4-羟基-3-甲氧基吲哚吗啡喃类似物的δ阿片样物质亲和力和选择性
J Med Chem. 1999 May 6;42(9):1673-9. doi: 10.1021/jm9807003.
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Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.运用信息-位点概念设计肽模拟物δ阿片受体拮抗剂
J Med Chem. 1990 Jun;33(6):1714-20. doi: 10.1021/jm00168a028.
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