A Novel Series of Piperidin-4-yl-1,3-Dihydroindol-2-ones as Agonist and Antagonist Ligands at the Nociceptin Receptor

Nurulain T. Zaveri; Faming Jiang; Cris M. Olsen; Jeffrey R. Deschamps; Damon Parrish; Willma Polgar; Lawrence Toll

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A Novel Series of Piperidin-4-yl-1,3-Dihydroindol-2-ones as Agonist and Antagonist Ligands at the Nociceptin Receptor

机译：一个新型的哌啶丁-4-基-1,3-二氢吲哚-2-酮作为痛觉敏受体的激动剂和拮抗剂配体。

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A series of N-(4-piperidinyl)-2-indolinones were discovered as a new structural class of nociceptin receptor (NOP) ligands. Unlike other previously reported classes of NOP receptor ligands, modifications of the piperidine N substituents afforded both potent agonists and antagonists, with modest selectivities over other opioid receptors. The SAR revealed in this new series will provide important insights for the development of pharmacophores for agonist and antagonist actions at the NOP receptor.

机译：发现一系列N-（4-哌啶基）-2-吲哚满酮是伤害感受素受体（NOP）配体的新结构类别。与以前报道的其他类型的NOP受体配体不同，哌啶N取代基的修饰提供了有效的激动剂和拮抗剂，对其他阿片受体的选择性适中。这个新系列中揭示的SAR将为药效基团对NOP受体的激动剂和拮抗剂作用的开发提供重要见解。

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《Journal of Medicinal Chemistry》 |2004年第12期|共4页
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Nurulain T. Zaveri; Faming Jiang; Cris M. Olsen; Jeffrey R. Deschamps; Damon Parrish; Willma Polgar; Lawrence Toll;
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1. A Novel Series of Piperidin-4-yl-1,3-Dihydroindol-2-ones as Agonist and Antagonist Ligands at the Nociceptin Receptor [J] . Nurulain T. Zaveri, Faming Jiang, Cris M. Olsen, Journal of Medicinal Chemistry . 2004,第12期

机译：一个新型的哌啶丁-4-基-1,3-二氢吲哚-2-酮作为痛觉敏受体的激动剂和拮抗剂配体。
2. The nociceptin orphanin FQ peptide receptor agonist, Ro64-6198, impairs recognition memory formation through interaction with glutamatergic but not cholinergic receptor antagonists [J] . ReissD., PrinssenE.P., WichmannJ., Neurobiology of learning and memory . 2012,第3期

机译：Nociceptin Orphanin FQ肽受体激动剂Ro64-6198通过与谷氨酸能受体而非胆碱能受体拮抗剂相互作用而损害识别记忆的形成
3. Agonist/antagonist modulation in a series of 2-aryl benzimidazole H4 receptor ligands. [J] . Savall BM, Edwards JP, Venable JD, Bioorganic and Medicinal Chemistry Letters . 2010,第11期

机译：一系列2-芳基苯并咪唑H4受体配体中的激动剂/拮抗剂调制。
4. Identification of opioid receptor ligand interactions using structurally related delta-opioid receptor agonists and antagonists and molecular modeling. [C] . Sharon D.Bryant, Yunden Jinsmaa, Lawrence H.Lazarus International Peptide Symposium;European Peptide Symposium . 2005

机译：使用结构相关的δ-阿片类受体激动剂和拮抗剂和分子建模鉴定阿片受体配体的相互作用。
5. Bifunctional Mu Opioid and Nociceptin/Orphanin FQ Receptor Agonist BU08028 Selectively Decreases Alcohol Drinking in Rhesus Monkeys [D] . Flynn, Shawn M. 2019

机译：双功能Mu阿片类和Noceptin / Orphanin FQ受体激动剂BU08028选择性减少恒河猴的饮酒量
6. A Novel Series of Piperidin-4-yl-13-Dihydroindol-2-ones as Agonist and Antagonist Ligands at the Nociceptin Receptor [O] . Nurulain T. Zaveri, Faming Jiang, Cris M. Olsen, -1

机译：一个新型的哌啶丁-4-基-13-二氢吲哚-2-酮作为伤害感受器受体上的激动剂和拮抗剂配体。
7. Evidence that [Phe1 ψ(CH2-NH)Gly2]nociceptin-(1-13)-NH2, a peripheral ORL-1 receptor antagonist, acts as an agonist in the rat spinal cord [O] . Carpenter, Kate J, Dickenson, Anthony H 1998

机译：周围的ORL-1受体拮抗剂[Phe1ψ（CH2-NH）Gly2] nociceptin-（1-13）-NH2在大鼠脊髓中起激动剂作用的证据

A Novel Series of Piperidin-4-yl-1,3-Dihydroindol-2-ones as Agonist and Antagonist Ligands at the Nociceptin Receptor

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