Literature DB >> 10602690

Discovery of the first potent and selective small molecule opioid receptor-like (ORL1) antagonist: 1-[(3R,4R)-1-cyclooctylmethyl-3- hydroxymethyl-4-piperidyl]-3-ethyl-1, 3-dihydro-2H-benzimidazol-2-one (J-113397).

H Kawamoto1, S Ozaki, Y Itoh, M Miyaji, S Arai, H Nakashima, T Kato, H Ohta, Y Iwasawa.   

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Year:  1999        PMID: 10602690     DOI: 10.1021/jm990517p

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


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1.  Enhanced spinal nociceptin receptor expression develops morphine tolerance and dependence.

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Journal:  J Neurosci       Date:  2000-10-15       Impact factor: 6.167

2.  Inhibition of striatal and retinal dopamine release via nociceptin/orphanin FQ receptors.

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Journal:  Br J Pharmacol       Date:  2002-12       Impact factor: 8.739

Review 3.  Nociceptin Opioid Receptor (NOP) as a Therapeutic Target: Progress in Translation from Preclinical Research to Clinical Utility.

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4.  Presynaptic opioid receptors on noradrenergic and serotonergic neurons in the human as compared to the rat neocortex.

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5.  A new synthesis of the ORL-1 antagonist 1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidinyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one (J-113397) and activity in a calcium mobilization assay.

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6.  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
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7.  The design and synthesis of a novel quinolizidine template for potent opioid and opioid receptor-like (ORL1, NOP) receptor ligands.

Authors:  Ling Jong; Nurulain Zaveri; Lawrence Toll
Journal:  Bioorg Med Chem Lett       Date:  2004-01-05       Impact factor: 2.823

8.  Buprenorphine: a unique drug with complex pharmacology.

Authors:  Kabirullah Lutfy; Alan Cowan
Journal:  Curr Neuropharmacol       Date:  2004-10       Impact factor: 7.363

Review 9.  Nociceptin/Orphanin FQ Receptor Structure, Signaling, Ligands, Functions, and Interactions with Opioid Systems.

Authors:  Lawrence Toll; Michael R Bruchas; Girolamo Calo'; Brian M Cox; Nurulain T Zaveri
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10.  Buprenorphine reduces alcohol drinking through activation of the nociceptin/orphanin FQ-NOP receptor system.

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