NOP Ligands for the Treatment of Anxiety and Mood Disorders

Gavioli, Elaine C.; Holanda, Victor A.D.; Ruzza, Chiara

doi:10.1007/164_2018_188

Cited by 17 publications

(13 citation statements)

References 95 publications

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“…The antidepressant like effects of BTRX-246040 where then confirmed in the LH model of depression, where it reversed the LH acquired behavior after one single administration. This effect of BTRX-246040 is similar to those reported for the classical NOP antagonists UFP-101 and SB-612111 (Holanda et al, 2016) and corroborates the widely recognized hypothesis that the blockage of the NOP receptor produces antidepressant effects in rodents subjected to different models of depression (Gavioli and Calo', 2013;Gavioli et al, 2019;Witkin et al, 2014). Of note, only one acute administration of BTRX-246040 was able to produce antidepressant effects in the LH model.…”

Section: Discussionsupporting

confidence: 86%

“…This peptide is the endogenous ligand of an inhibitory G protein coupled receptor named N/OFQ peptide receptor (NOP) (Meunier et al, 1995;Reinscheid et al, 1995). Clinical and preclinical findings suggest that the blockade of the NOP signaling induces antidepressant-like effects (Gavioli and Calo', 2013;Gavioli et al, 2019;Post et al, 2016b).…”

Section: Introductionmentioning

confidence: 99%

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The NOP antagonist BTRX-246040 increases stress resilience in mice without affecting adult neurogenesis in the hippocampus

et al. 2022

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Section: Discussionsupporting

confidence: 86%

Section: Introductionmentioning

confidence: 99%

The NOP antagonist BTRX-246040 increases stress resilience in mice without affecting adult neurogenesis in the hippocampus

et al. 2022

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“…and UFP-101 (1.0–10 nmol, i.c.v.) attenuated depressive-like symptoms in the mouse learned helplessness model [ 170 , 174 , 175 ]. Furthermore, UFP-101(10 nmol, i.c.v.)…”

Section: Role Of the N/ofq-nop Receptor System In Anxiety And Mood Disordersmentioning

confidence: 99%

Role of Nociceptin/Orphanin FQ-NOP Receptor System in the Regulation of Stress-Related Disorders

Ubaldi

Cannella

Borruto

et al. 2021

IJMS

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Nociceptin/orphanin FQ (N/OFQ) is a 17-residue neuropeptide that binds the nociceptin opioid-like receptor (NOP). N/OFQ exhibits nucleotidic and aminoacidics sequence homology with the precursors of other opioid neuropeptides but it does not activate either MOP, KOP or DOP receptors. Furthermore, opioid neuropeptides do not activate the NOP receptor. Generally, activation of N/OFQ system exerts anti-opioids effects, for instance toward opioid-induced reward and analgesia. The NOP receptor is widely expressed throughout the brain, whereas N/OFQ localization is confined to brain nuclei that are involved in stress response such as amygdala, BNST and hypothalamus. Decades of studies have delineated the biological role of this system demonstrating its involvement in significant physiological processes such as pain, learning and memory, anxiety, depression, feeding, drug and alcohol dependence. This review discusses the role of this peptidergic system in the modulation of stress and stress-associated psychiatric disorders in particular drug addiction, mood, anxiety and food-related associated-disorders. Emerging preclinical evidence suggests that both NOP agonists and antagonists may represent a effective therapeutic approaches for substances use disorder. Moreover, the current literature suggests that NOP antagonists can be useful to treat depression and feeding-related diseases, such as obesity and binge eating behavior, whereas the activation of NOP receptor by agonists could be a promising tool for anxiety.

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“…This peptide is the endogenous ligand of an inhibitory G proteincoupled receptor named N/OFQ peptide receptor (NOP) (Meunier et al, 1995;Reinscheid et al, 1995). Considering the wide brain expression of the peptide and its receptor, particularly in areas related to emotional processing and stress, such as amygdala, hippocampus, hypothalamus, bed nucleus of stria terminalis, and brainstem monoaminergic nuclei (Boom et al, 1999;Mollereau and Mouledous, 2000;Neal et al, 1999aNeal et al, , 1999b, it was initially suggested that this peptidergic system might play a regulatory role in stress-related psychiatric disorders, such as major depression, anxiety, drug abuse, and food consumptionrelated disorders (Gavioli and Calo' 2013;Gavioli et al, 2018;Toll et al, 2016;Witkin et al, 2016).…”

Section: Introductionmentioning

confidence: 99%

Modulation of the NOP receptor signaling affects resilience to acute stress

et al. 2019

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Background: The peptide nociceptin/orphanin FQ (N/OFQ) and its receptor (NOP) are implicated in the modulation of emotional states. Previous human and rodent findings support NOP antagonists as antidepressants. However, the role played by the N/OFQ–NOP receptor system in resilience to stress is unclear. Aims: The present study investigated the effects of activation or blockade of NOP receptor signaling before exposure to acute stress. Methods: The behavioral effects of the administration before stress of the NOP agonists Ro 65-6570 (0.01–1 mg/kg) and MCOPPB (0.1–10 mg/kg), and the NOP antagonist SB-612111 (1–10 mg/kg) were assessed in mice exposed to inescapable electric footshock and forced swim as stressors. The behavioral phenotype of mice lacking the NOP receptor (NOP(-/-)) exposed to inescapable electric footshock was also investigated. Results: The activation of NOP receptor signaling with the agonists increased the percentage of mice developing helpless behavior and facilitated immobile posture. In contrast, the blockade of NOP receptor reduced the acquisition of depressive-like phenotypes, and similar resistance to develop helpless behaviors was observed in NOP(-/-) mice. Under the same stressful conditions, the antidepressant nortriptyline (20 mg/kg) did not change the acquisition of helpless behavior and immobile posture. Conclusions: These findings support the view that NOP activation during acute stress facilitates the development of depressive-related behaviors, whereas NOP blockade has a protective outcome. This study showed for first time that NOP antagonists are worthy of investigation as preemptive treatments in patients with severe risk factors for depression.

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NOP Ligands for the Treatment of Anxiety and Mood Disorders

Cited by 17 publications

References 95 publications

The NOP antagonist BTRX-246040 increases stress resilience in mice without affecting adult neurogenesis in the hippocampus

The NOP antagonist BTRX-246040 increases stress resilience in mice without affecting adult neurogenesis in the hippocampus

Role of Nociceptin/Orphanin FQ-NOP Receptor System in the Regulation of Stress-Related Disorders

Modulation of the NOP receptor signaling affects resilience to acute stress

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