Literature DB >> 15163178

A novel series of piperidin-4-yl-1,3-dihydroindol-2-ones as agonist and antagonist ligands at the nociceptin receptor.

Nurulain T Zaveri1, Faming Jiang, Cris M Olsen, Jeffrey R Deschamps, Damon Parrish, Willma Polgar, Lawrence Toll.   

Abstract

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.

Entities:  

Mesh：

Substances：

Year:  2004        PMID： 15163178      PMCID： PMC3852901          DOI： 10.1021/jm034249d

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  23 in total

1.  Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.

Authors:  L Toll; I P Berzetei-Gurske; W E Polgar; S R Brandt; I D Adapa; L Rodriguez; R W Schwartz; D Haggart; A O'Brien; A White; J M Kennedy; K Craymer; L Farrington; J S Auh
Journal:  NIDA Res Monogr       Date:  1998-03

2.  Facilitation of long-term potentiation and memory in mice lacking nociceptin receptors.

Authors:  T Manabe; Y Noda; T Mamiya; H Katagiri; T Houtani; M Nishi; T Noda; T Takahashi; T Sugimoto; T Nabeshima; H Takeshima
Journal:  Nature       Date:  1998-08-06       Impact factor: 49.962

3.  Relationship between binding affinity and functional activity of nociceptin/orphanin FQ.

Authors:  I D Adapa; L Toll
Journal:  Neuropeptides       Date:  1997-10       Impact factor: 3.286

4.  Intracerebroventricular orphanin FQ/nociceptin suppresses dopamine release in the nucleus accumbens of anaesthetized rats.

Authors:  N P Murphy; H T Ly; N T Maidment
Journal:  Neuroscience       Date:  1996-11       Impact factor: 3.590

5.  Inhibitory effect of nociceptin on [3H]-5-HT release from rat cerebral cortex slices.

Authors:  A Siniscalchi; D Rodi; L Beani; C Bianchi
Journal:  Br J Pharmacol       Date:  1999-09       Impact factor: 8.739

6.  Orphanin FQ acts as an anxiolytic to attenuate behavioral responses to stress.

Authors:  F Jenck; J L Moreau; J R Martin; G J Kilpatrick; R K Reinscheid; F J Monsma; H P Nothacker; O Civelli
Journal:  Proc Natl Acad Sci U S A       Date:  1997-12-23       Impact factor: 11.205

7.  Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1.

Authors:  C T Dooley; C G Spaeth; I P Berzetei-Gurske; K Craymer; I D Adapa; S R Brandt; R A Houghten; L Toll
Journal:  J Pharmacol Exp Ther       Date:  1997-11       Impact factor: 4.030

8.  Orphanin FQ, a novel neuropeptide with anti-stress-like activity.

Authors:  G Griebel; G Perrault; D J Sanger
Journal:  Brain Res       Date:  1999-07-31       Impact factor: 3.252

9.  Orphanin FQ/nociceptin blocks acquisition of morphine place preference.

Authors:  N P Murphy; Y Lee; N T Maidment
Journal:  Brain Res       Date:  1999-06-19       Impact factor: 3.252

10.  Enhancement of spatial attention in nociceptin/orphanin FQ receptor-knockout mice.

Authors:  T Mamiya; Y Noda; M Nishi; H Takeshima; T Nabeshima
Journal:  Brain Res       Date:  1998-02-09       Impact factor: 3.252
View more
  26 in total

1.  Small-molecule nociceptin receptor agonist ameliorates mast cell activation and pain in sickle mice.

Authors:  Derek Vang; Jinny A Paul; Julia Nguyen; Huy Tran; Lucile Vincent; Dennis Yasuda; Nurulain T Zaveri; Kalpna Gupta
Journal:  Haematologica       Date:  2015-08-20       Impact factor: 9.941

Review 2.  Nociceptin Opioid Receptor (NOP) as a Therapeutic Target: Progress in Translation from Preclinical Research to Clinical Utility.

Authors:  Nurulain T Zaveri
Journal:  J Med Chem       Date:  2016-03-14       Impact factor: 7.446

3.  In silico study of the structurally similar ORL1 receptor agonist and antagonist pairs reveal possible mechanism of receptor activation.

Authors:  Milan Senćanski; Ljiljana Dosen-Mićović
Journal:  Protein J       Date:  2014-06       Impact factor: 2.371

4.  Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP-receptor selective scaffolds. Part II.

Authors:  V Blair Journigan; Willma E Polgar; Taline V Khroyan; Nurulain T Zaveri
Journal:  Bioorg Med Chem       Date:  2014-03-05       Impact factor: 3.641

5.  A bifunctional nociceptin and mu opioid receptor agonist is analgesic without opioid side effects in nonhuman primates.

Authors:  Huiping Ding; Norikazu Kiguchi; Dennis Yasuda; Pankaj R Daga; Willma E Polgar; James J Lu; Paul W Czoty; Shiroh Kishioka; Nurulain T Zaveri; Mei-Chuan Ko
Journal:  Sci Transl Med       Date:  2018-08-29       Impact factor: 17.956

6.  Anti-Parkinsonian and anti-dyskinetic profiles of two novel potent and selective nociceptin/orphanin FQ receptor agonists.

Authors:  Ludovico Arcuri; Salvatore Novello; Martina Frassineti; Daniela Mercatelli; Clarissa Anna Pisanò; Ilaria Morella; Stefania Fasano; Blair V Journigan; Michael E Meyer; Willma E Polgar; Riccardo Brambilla; Nurulain T Zaveri; Michele Morari
Journal:  Br J Pharmacol       Date:  2018-01-31       Impact factor: 8.739

7.  Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP receptor-selective scaffolds. Part I.

Authors:  Nurulain T Zaveri; Faming Jiang; Cris Olsen; Willma E Polgar; Lawrence Toll
Journal:  Bioorg Med Chem Lett       Date:  2013-04-04       Impact factor: 2.823

8.  Differential effects of nociceptin/orphanin FQ (NOP) receptor agonists in acute versus chronic pain: studies with bifunctional NOP/μ receptor agonists in the sciatic nerve ligation chronic pain model in mice.

Authors:  Taline V Khroyan; Willma E Polgar; Juan Orduna; Jose Montenegro; Faming Jiang; Nurulain T Zaveri; Lawrence Toll
Journal:  J Pharmacol Exp Ther       Date:  2011-08-22       Impact factor: 4.030

9.  Comparison of the antinociceptive and antirewarding profiles of novel bifunctional nociceptin receptor/mu-opioid receptor ligands: implications for therapeutic applications.

Authors:  Lawrence Toll; Taline V Khroyan; Willma E Polgar; Faming Jiang; Cris Olsen; Nurulain T Zaveri
Journal:  J Pharmacol Exp Ther       Date:  2009-09-22       Impact factor: 4.030

10.  Activity of new NOP receptor ligands in a rat peripheral mononeuropathy model: potentiation of morphine anti-allodynic activity by NOP receptor antagonists.

Authors:  Taline V Khroyan; Willma E Polgar; Juan Orduna; Faming Jiang; Cris Olsen; Lawrence Toll; Nurulain T Zaveri
Journal:  Eur J Pharmacol       Date:  2009-03-12       Impact factor: 4.432
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.