ReviewCNS drug reviews2007
The pharmacology of Ro 64-6198, a systemically active, nonpeptide NOP receptor (opiate receptor-like 1, ORL-1) agonist with diverse preclinical therapeutic activity.
Review in CNS drug reviews, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
18 citing papers in PubMed, 50 citations in OpenAlex.
- NOP agonist AT-403 promoted sleep in lactic acid-induced acute pain model.Frontiers in pain research (Lausanne, Switzerland) · 2025Article
- Review
- Spotlight on Nociceptin/Orphanin FQ Receptor in the Treatment of Pain.Molecules (Basel, Switzerland) · 2022Review
- Biased Opioid Ligands.Molecules (Basel, Switzerland) · 2020Review
- Analysis of the distribution of spinal NOP receptors in a chronic pain model using NOP-eGFP knock-in mice.British journal of pharmacology · 2018Article
- Targeting multiple opioid receptors - improved analgesics with reduced side effects?British journal of pharmacology · 2018Review
- In vitro functional characterization of novel nociceptin/orphanin FQ receptor agonists in recombinant and native preparations.European journal of pharmacology · 2016Article
- Beta-arrestin 2 rather than G protein efficacy determines the anxiolytic-versus antidepressant-like effects of nociceptin/orphanin FQ receptor ligands.Neuropharmacology · 2016Article
- Nociceptin/Orphanin FQ Receptor Structure, Signaling, Ligands, Functions, and Interactions with Opioid Systems.Pharmacological reviews · 2016Review
- Novel Synthesis and Pharmacological Characterization of NOP Receptor Agonist 8-[(1S,3aS)-2,3,3a,4,5,6-Hexahydro-1H-phenalen-1-yl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one (Ro 64-6198).ACS chemical neuroscience · 2015Article
- In vitro and in vivo pharmacological characterization of nociceptin/orphanin FQ tetrabranched derivatives.British journal of pharmacology · 2014Article
- Select G-protein-coupled receptors modulate agonist-induced signaling via a ROCK, LIMK, and β-arrestin 1 pathway.Cell reports · 2013Article
- Further characterization of the prototypical nociceptin/orphanin FQ peptide receptor agonist Ro 64-6198 in rodent models of conflict anxiety and despair.Psychopharmacology · 2012Article
- UFP-112 a potent and long-lasting agonist selective for the Nociceptin/Orphanin FQ receptor.CNS neuroscience & therapeutics · 2011Review
- The effects of nociceptin/orphanin FQ receptor agonist Ro 64-6198 and diazepam on antinociception and remifentanil self-administration in rhesus monkeys.Psychopharmacology · 2011Article
- Behavioral effects of a synthetic agonist selective for nociceptin/orphanin FQ peptide receptors in monkeys.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2009Article
- Pharmacological profile of NOP receptors coupled with calcium signaling via the chimeric protein G alpha qi5.Naunyn-Schmiedeberg's archives of pharmacology · 2009Article
- Orphan GPCR research.British journal of pharmacology · 2008Review
Corrections and comments
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Authors and funding
1 author at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The NOP receptor (formerly referred to as opiate receptor-like 1, ORL-1, LC132, OP(4), or NOP(1)) is a G protein-coupled receptor that shares high homology to the classic opioid MOP, DOP, and KOP (mu, delta, and kappa, respectively) receptors and was first cloned in 1994 by several groups. The NOP receptor remained an orphan receptor until 1995, when the endogenous neuropeptide agonist, known as nociceptin or orphanin FQ (N/OFQ) was isolated. Five years later, a group at Hoffmann-La Roche reported on the selective, nonpeptide NOP agonist Ro 64-6198, which became the most extensively published nonpeptide NOP agonist and a valuable pharmacological tool in determining the potential of the NOP receptor as a therapeutic target. Ro 64-6198 is systemically active and achieves high brain penetration. It has subnanomolar affinity for the NOP receptor and is at least 100 times more selective for the NOP receptor over the classic opioid receptors. Ro 64-6198 ranges from partial to full agonist, depending on the assay. Preclinical data indicate that Ro 64-6198 may have broad clinical uses, such as in treating stress and anxiety, addiction, neuropathic pain, cough, and anorexia. This review summarizes the pharmacology and preclinical data of Ro 64-6198.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.