Article
Pharmacology & Pharmacy
Sonny H. J. Sliepen, Johanna Korioth, Thomas Christoph, Thomas M. Tzschentke, Marta Diaz-delCastillo, Anne-Marie Heegaard, Kris Rutten
Summary: This study investigated the analgesic potential of NOP receptor activation in a rodent cancer-induced bone pain model, finding that Nociceptin and Ro65-6570 could inhibit cancer-induced mechanical allodynia, with J-113397 selectively antagonizing the effect of Ro65-6570. Additionally, MRMT-1/Luc2-bearing animals showed elevated plasma cytokine levels and altered expression of NOP-r gene in DRG and bone marrow.
BRITISH JOURNAL OF PHARMACOLOGY
(2021)
Review
Biochemistry & Molecular Biology
Massimo Ubaldi, Nazzareno Cannella, Anna Maria Borruto, Michele Petrella, Maria Vittoria Micioni Di Bonaventura, Laura Soverchia, Serena Stopponi, Friedbert Weiss, Carlo Cifani, Roberto Ciccocioppo
Summary: Nociceptin/orphanin FQ (N/OFQ) is a neuropeptide that binds the NOP receptor and exerts anti-opioids effects; the NOP receptor is widely expressed in the brain, while N/OFQ is mainly localized in stress-related brain nuclei; preclinical evidence suggests that both NOP agonists and antagonists may be effective therapeutic approaches for substance use disorders.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Pharmacology & Pharmacy
Clarissa A. Pisano, Daniela Mercatelli, Martina Mazzocchi, Alberto Brugnoli, Ilaria Morella, Stefania Fasano, Nurulain T. Zaveri, Riccardo Brambilla, Gerard W. O'Keeffe, Richard R. Neubig, Michele Morari
Summary: The study indicates that RGS4 physiologically inhibits NOP receptor signaling and the chemical probe CCG-203920 can enhance NOP responses and improve the antidyskinetic potential of NOP receptor agonists.
BRITISH JOURNAL OF PHARMACOLOGY
(2023)
Review
Biochemistry & Molecular Biology
Amal El Daibani, Tao Che
Summary: In our society today, pain has become a significant source of strain on individuals. Developing new pain treatments with fewer adverse effects is crucial. The NOP receptor has emerged as a promising focal point for novel pain therapies, offering an alternative to opioid morphine with potential life-threatening effects and addiction. This article reviews the molecular and cellular structure controlling the cellular trafficking of the NOP receptor and presents studies supporting its role in pain management.
Article
Psychiatry
Fangmin Wang, Wenwen Shen, Yujia Cai, Xin Zhang, Han Du, Miaojun Lai, Huifen Liu, Evelyne Kohli, Wenhua Zhou
Summary: Buprenorphine can reduce METH intake and drug-seeking behavior by activating NOP receptors.
FRONTIERS IN PSYCHIATRY
(2022)
Article
Pharmacology & Pharmacy
Mark F. Bird, Christopher P. Hebbes, Anushuya Tamang, Jonathon Mark Willets, Jonathan P. Thompson, Remo Guerrini, Girolamo Calo, David G. Lambert
Summary: In this study, the role of N/OFQ-NOP system was explored in freshly isolated volunteer human B- and T-cells incubated with LPS and PepG as a model of in vitro sepsis. The findings suggest that N/OFQ-NOP receptors play a regulatory role in B and T cell function, inhibiting cell migration and reducing GM-CSF release to variable degrees.
BRITISH JOURNAL OF PHARMACOLOGY
(2023)
Article
Multidisciplinary Sciences
Stephen R. Morairty, Yu Sun, Lawrence Toll, Michael R. Bruchas, Thomas S. Kilduff
Summary: This study evaluated the effects of two NOPR agonists on sleep/wake in rats, mice, and Cynomolgus macaques. The results showed that these agonists increased non-Rapid Eye Movement sleep and electroencephalogram slow wave activity, while suppressing Rapid Eye Movement sleep in all three species. These findings suggest that the N/OFQ-NOPR system may have a previously unrecognized role in sleep/wake control and could be a potential therapeutic target for insomnia.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2023)
Review
Pharmacology & Pharmacy
Omar N. Al Yacoub, Hibah O. Awwad, Yong Zhang, Kelly M. Standifer
Summary: This article reviews the role of the N/OFQ-NOP receptor system in the neurological and behavioral sequelae of PTSD and TBI. The current findings suggest that NOP modulators may have potential as therapeutics for these disorders and their co-morbidities. The authors advocate for the development of standards for common data elements reporting to improve reproducibility and data sharing.
PHARMACOLOGY & THERAPEUTICS
(2022)
Article
Biochemistry & Molecular Biology
Elaine C. Gavioli, Victor A. D. Holanda, Girolamo Calo, Chiara Ruzza
Summary: Resilience plays a crucial role in mental health, and understanding its mechanisms can improve treatment outcomes and help high-risk individuals. The N/OFQ-NOP system is central to stress response, affecting hormone secretion, behavior, and psychopathologies.
Article
Neurosciences
Wenfu Li, Zhiheng Ren, Ying Tang, Yixin Fu, Shizhu Sun, Ruxuan Ding, Jiawei Hou, Yunlin Mai, Bo Zhan, Yingxin Zhu, Wanhong Zuo, Jiang-Hong Ye, Rao Fu
Summary: Recent studies suggest that the stimulation of the rostromedial tegmental nucleus (RMTg) and the role of the nociceptin/orphanin FQ (N/OFQ) system may be involved in affective disorders and drug addiction. This study found that N/OFQ signaling contributes to changes in behavior and RMTg activity of rats during alcohol withdrawal. The deficiency of RMTg N/OFQ signaling mediates anxiety- and depression-like behaviors in alcohol withdrawn rats, and the intervention of the N/OFQ system may potentially help individuals with alcohol use disorders.
NEUROPSYCHOPHARMACOLOGY
(2023)
Article
Multidisciplinary Sciences
Mark F. Bird, Barbara Gallacher-Horley, John McDonald, David G. McVey, Fatin Al-Janabi, Remo Guerrini, Girolamo Calo, Shu Ye, Jonathan P. Thompson, David G. Lambert
Summary: Sepsis is a dysregulated host response to infection that can cause widespread effects on other organs. The study found that N/OFQ receptors are expressed on immune cells and vascular endothelial cells, and LPS/PepG treatment increases functional expression of NOP receptors in vascular endothelium. These findings may contribute to our understanding of the hypotensive response in sepsis and provide new therapeutic targets for its treatment.
Review
Pharmacology & Pharmacy
Huiping Ding, Norikazu Kiguchi, MaryBeth Dobbins, E. Alfonso Romero-Sandoval, Shiroh Kishioka, Mei-Chuan Ko
Summary: As currently available opioid analgesics often have dose-limiting adverse effects, new approaches have been pursued to develop safe and non-addictive pain medications. NOP receptor-related agonists have emerged as a promising target for developing novel opioids that modulate the analgesic and addictive properties of MOP receptor agonists. Several lines of evidence suggest that peptidic and non-peptidic NOP receptor agonists and mixed NOP/MOP receptor partial agonists show potent analgesic effects in experimental animal models without eliciting adverse effects.
Article
Biochemistry & Molecular Biology
Zhihui Zhou, Jie He, Feiyi Yang, Qingshan Pan, Zunhua Yang, Pengwu Zheng, Shan Xu, Wufu Zhu
Summary: A new class of quinazoline derivatives as EGFR inhibitors was designed and synthesized, with compound 9e showing promising inhibitory activity and specificity, suggesting potential therapeutic value against lung cancer cells.
BIOORGANIC CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Omar N. Al Yacoub, Stefano Tarantini, Yong Zhang, Anna Csiszar, Kelly M. Standifer
Summary: Traumatic brain injury (TBI) affects millions of people each year and is a leading cause of death and disability. This study suggests that the N/OFQ-NOP receptor pathway plays a significant role in regulating cerebral blood flow and injury markers in TBI, indicating that the NOP receptor could be a potential therapeutic target for TBI.
FRONTIERS IN PHARMACOLOGY
(2023)
Article
Neurosciences
Sarah Sayers, Nikki Le, Jennifer Hernandez, Veronica Mata-Pacheco, Edward J. Wagner
Summary: N/OFQ(ARC) neurons play a vital role in promoting rebound hyperphagia by inhibiting anorexigenic neural substrates under negative energy balance conditions, an effect that is diminished by E-2 in females.
JOURNAL OF PHYSIOLOGY-LONDON
(2022)