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NOP-Related Mechanisms in Substance Use Disorders
Nociceptin/orphanin FQ (N/OFQ) is a 17 amino acid peptide that was deorphanized in 1995 and has been widely studied since. The role of the N/OFQ... -
Electrophysiological Actions of N/OFQ
Whilst the nociceptin/orphanin FQ (N/OFQ) receptor (NOP) has similar intracellular coupling mechanisms to opioid receptors, it has distinct... -
Interactive Mechanisms of Supraspinal Sites of Opioid Analgesic Action: A Festschrift to Dr. Gavril W. Pasternak
Almost a half century of research has elaborated the discoveries of the central mechanisms governing the analgesic responses of opiates, including...
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NOP-Targeted Nonpeptide Ligands
The development of nonpeptide systemically active small-molecule NOP-targeted ligands has contributed tremendously to validating the NOP receptor as... -
Opioids and Opiates: Pharmacology, Abuse, and Addiction
This chapter presents an overview of the opioid system consisting of a wide variety of endogenous and exogenous ligands, as well as several receptor... -
Understanding Opioid Actions, Pain and Analgesia: A Tribute to Dr. Gavril Pasternak
This special issue is a tribute to our mentor, colleague and friend, Gavril W. Pasternak, MD, PhD. Homage to the breadth and depth of his work (~ 450...
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Opioid Agonists and Antagonists
Pain causes severe limitation of human functionality and productivity. Humans have waged a long war against pain using different forms of analgesics.... -
Fear expression is reduced after acute and repeated nociceptin/orphanin FQ (NOP) receptor antagonism in rats: therapeutic implications for traumatic stress exposure
RationaleEvaluation of pharmacotherapies for acute stress disorder (ASD) or post-traumatic stress disorder (PTSD) is challenging due to robust...
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NOP agonists prevent the antidepressant-like effects of nortriptyline and fluoxetine but not R-ketamine
RationaleNociceptin/orphanin FQ (N/OFQ) is the endogenous ligand of a Gi protein-coupled receptor named NOP. Both N/OFQ and NOP receptor are widely...
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Blockade of NOP receptor modulates anxiety-related behaviors in mice exposed to inescapable stress
RationaleDepression and anxiety frequently co-occur, and this has important clinical implications. Previous studies showed that activation of the...
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Opioid toxicity: histamine, hypersensitivity, and MRGPRX2
Insights into the pathophysiology of many non-immune-mediated drug reactions referred to as toxicities, sensitivities, intolerances, or...
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Pharmacology of Endogenous Opioids, Opiates and Their Receptors
The search for analgesia is the main drive for the discovery of opioid receptors and their endogenous ligand peptides. Although opioid peptides are... -
The History of N/OFQ and the NOP Receptor
The discovery of nociceptin/orphanin FQ (N/OFQ) marks the genuine start of the reverse pharmacology era, when systematic hunting for ligands of... -
Preclinical Models of Stress and Environmental Influences on Binge Eating
Preclinical models cannot explain all of the complex internal and external factors that influence eating behaviors in humans. Still, they represent... -
Pharmacological modulation of conditioned fear in the fear-potentiated startle test: a systematic review and meta-analysis of animal studies
Rationale and objectivesFear conditioning is an important aspect in the pathophysiology of anxiety disorders. The fear-potentiated startle test is...
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NOP Ligands for the Treatment of Anxiety and Mood Disorders
Many studies point toward the nociceptin/orphanin FQ (N/OFQ) and the N/OFQ peptide receptor (NOP) as targets for the development of innovative drugs... -
NOP-Targeted Peptide Ligands
The nociceptin/orphanin FQ (N/OFQ)-N/OFQ peptide (NOP) receptor system is widely distributed at both the peripheral and central level where it... -
The Nociceptin/Orphanin FQ System and the Regulation of Memory
Nociceptin/orphanin FQ (N/OFQ) is an endogenous neuropeptide of 17 amino acids, related to opioid peptides but with its own receptor, distinct from... -
Negative relationship between brain α1A-AR neurotransmission and βArr2 levels in anxious adolescent rats subjected to early life stress
Early-life stress is correlated with the development of anxiety-related behavior in adolescence, but underlying mechanisms remain poorly known. The α 1A...