Analgesic effect of intrathecally administered nociceptin, an opioid receptor-like1 receptor agonist, in the rat formalin test

Yamamoto, Tatsuo; Nozaki-Taguchi, Natsuko; Kimura, Sadao

doi:10.1016/s0306-4522(97)00166-8

Cited by 124 publications

(77 citation statements)

References 23 publications

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“…causes antinociceptive effects at high doses (nanogram to microgram range), Noc/OFQ produces pronociceptive and allodynic effects at low doses (femtogram to picogram range). Consistent with previous reports in rats (Erb et al, 1997;Yamamoto et al, 1997), the formalin-induced pain behaviors were blocked in mice by 1 g of Noc/OFQ (Fig. 5).…”

Section: Discussionsupporting

confidence: 92%

“…Similarly, whereas it facilitated the second phase of formalin-induced pain at a low dose of 10 pg, Noc/OFQ administered i.t. inhibited both the first-phase and secondphase pain behaviors in the formalin test at high doses of 0.3 to 3 g/mouse or 2 to 30 g/rat (Erb et al, 1997;Yamamoto et al, 1997;Nakano et al, 2000). Noc/OFQ was also reported to have no effect on its own (Vanderah et al, 1998).…”

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confidence: 99%

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Characterization of Nociceptin/Orphanin FQ-Induced Pain Responses by the Novel Receptor AntagonistN-(4-Amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl) Benzamide Monohydrochloride

Muratani

Minami²,

Enomoto³

et al. 2002

J Pharmacol Exp Ther

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At the spinal level, nociceptin/orphanin FQ (Noc/OFQ) produces pronociceptive and allodynic effects at low doses (picogram range), while causing antinociceptive effects at high doses (microgram range). The discrepancy of pain modulation by Noc/OFQ at low and high doses raised a question whether Noc/OFQ exerted actions through the same Noc/OFQ receptor. In the present study, we examined the involvement of the Noc/OFQ receptor in pain responses with the novel nonpeptide antagonist N-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl) benzamide monohydrochloride (JTC-801). Allodynia and hyperalgesia evoked by intrathecal administration of Noc/OFQ (50 pg/mouse) were dose dependently blocked by simultaneous administration of JTC-801 with IC 50 values of 32.2 and 363 pg, respectively. JTC-801 did not induce allodynia by itself. Subcutaneous injection of formalin into a hindpaw evoked biphasic pain behaviors such as flinching and biting in mice. Noc/OFQ at 10 pg increased the second-phase pain behaviors evoked by 1% formalin, whereas it strongly inhibited both the first-phase and second-phase pain evoked by 2% formalin at 1 g. Although the pronociceptive effect by 10 pg of Noc/OFQ was dose dependently blocked by JTC-801 with an IC 50 value of 4.58 pg, the antinociceptive effects by 1 g of Noc/OFQ were not antagonized by JTC-801. Furthermore, both phases of 2% formalin-induced pain behaviors were relieved by JTC-801. These results demonstrate that pronociceptive responses induced by a low dose of Noc/OFQ may be mediated through the Noc/OFQ receptor in the spinal cord and that JTC-801 can be a useful antagonist to examine the involvement of endogenous Noc/OFQ and mediation of the Noc/OFQ receptor under physiological and pathophysiological conditions including pain.

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Section: Discussionsupporting

confidence: 92%

mentioning

confidence: 99%

Characterization of Nociceptin/Orphanin FQ-Induced Pain Responses by the Novel Receptor AntagonistN-(4-Amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl) Benzamide Monohydrochloride

Muratani

Minami²,

Enomoto³

et al. 2002

J Pharmacol Exp Ther

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“…Although the antianalgesic effects of NOP receptor agonists delivered into the brain are very profound, the effect of N/OFQ administration into the spinal cord has the opposite result. Intrathecal administration of N/OFQ produces a direct antinociception and potentiates morphine (Xu et al, 1996;Yamamoto et al, 1997). …”

Section: Biologic Actions Of Nociceptin Opioid Peptide Receptorsmentioning

confidence: 99%

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

et al. 2016

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The NOP receptor (nociceptin/orphanin FQ opioid peptide receptor) is the most recently discovered member of the opioid receptor family and, together with its endogenous ligand, N/OFQ, make up the fourth members of the opioid receptor and opioid peptide family. Because of its more recent discovery, an understanding of the cellular and behavioral actions induced by NOP receptor activation are less well developed than for the other members of the opioid receptor family. All of these factors are important because NOP receptor activation has a clear modulatory role on mu opioid receptor-mediated actions and thereby affects opioid analgesia, tolerance development, and reward. In addition to opioid modulatory actions, NOP receptor activation has important effects on motor function and other physiologic processes. This review discusses how NOP pharmacology intersects, contrasts, and interacts with the mu opioid receptor in terms of tertiary structure and mechanism of receptor activation; location of receptors in the central nervous system; mechanisms of desensitization and downregulation; cellular actions; intracellular signal transduction pathways; and behavioral actions with respect to analgesia, tolerance, dependence, and reward. This is followed by a discussion of the agonists and antagonists that have most contributed to our current knowledge. Because NOP receptors are highly expressed in brain and spinal cord and NOP receptor activation sometimes synergizes with mu receptor-mediated actions and sometimes opposes them, an understanding of NOP receptor pharmacology in the context of these interactions with the opioid receptors will be crucial to the development of novel therapeutics that engage the NOP receptor

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“…administration of very low doses (0.005-0.05 nmoles; Florin et al, 1996). N/OFQ alters responses to nociceptive stimuli (Meunier et al, 1995;Reinscheid et al, 1995;Grisel et al, 1996;Erb et al, 1997;Hao et al, 1997;Helyes et al, 1997;King et al, 1997;Morgan et al, 1997;Tian et al, 1997;Yamamoto et al, 1997;Zhu et al, 1997). It appears not to exert any specific motivational actions in tests of place conditioning, when administered alone (Devine et al, 1996a;Ciccocioppo et al, 2000;Le Pen et al, 2002), but it stimulates feeding behavior (Pomonis et al, 1996;Stratford et al, 1997;Polidori et al, 2000;Ciccocioppo et al, 2002a), blocks morphine place conditioning (Murphy et al, 1999;Ciccocioppo et al, 2000), and interferes with the behaviorallyreinforcing effects of ethanol (Ciccocioppo et al, 1999(Ciccocioppo et al, , 2002bMartin-Fardon et al, 2000).…”

Section: Introductionmentioning

confidence: 99%

Nociceptin/Orphanin FQ Increases Anxiety-Related Behavior and Circulating Levels of Corticosterone During Neophobic Tests of Anxiety

Fernandez

Misilmeri

Felger

et al. 2003

Neuropsychopharmacol

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Intracranial administration of nociceptin/orphanin FQ (N/OFQ) increases circulating concentrations of adrenocorticotrophic hormone and corticosterone in unstressed rats, and elevates the responsiveness of these hormones during mild stress. Furthermore, N/OFQ and its cognate receptor are both abundant in a variety of limbic nuclei, and stress exposure decreases neuronal N/OFQ content in forebrain neurons. In light of these and other findings, we examined the potential involvement of N/OFQ in regulation of anxiety-related behaviors in rats. In the open field, elevated plus maze, and dark-light neophobic tests, intracerebroventricular N/OFQ (1.0 pmole-1.0 nmole) increased the expression of anxiety-related behaviors. Specifically, N/OFQ increased the latency to enter, decreased the number of entries into, and decreased the time spent in the exposed or brightly lit environments of all three tests. N/OFQ also enhanced thigmotactic responses in the open field test. The effects of diazepam and of the benzodiazepine inverse agonist FG 7142 were also assessed in independent groups of rats. In all three tests, the behavioral effects of N/OFQ resembled the anxiogenic actions of FG 7142, and contrasted with the anxiolytic actions of diazepam. N/OFQ administration also increased circulating concentrations of corticosterone during anxiety testing, in comparison with the concentrations in vehicle-treated controls. We conclude that N/OFQ administration is anxiogenic, and elevates responsiveness of the hypothalamic pituitary-adrenal axis during neophobic tests of anxiety. This supports the possibility that N/OFQ neurotransmission participates in processing of emotionally-salient and stressful stimuli, and suggests that normal functioning of the N/OFQ system may be important in physiological and psychological well-being.

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Analgesic effect of intrathecally administered nociceptin, an opioid receptor-like1 receptor agonist, in the rat formalin test

Cited by 124 publications

References 23 publications

Characterization of Nociceptin/Orphanin FQ-Induced Pain Responses by the Novel Receptor AntagonistN-(4-Amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl) Benzamide Monohydrochloride

Characterization of Nociceptin/Orphanin FQ-Induced Pain Responses by the Novel Receptor AntagonistN-(4-Amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl) Benzamide Monohydrochloride

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

Nociceptin/Orphanin FQ Increases Anxiety-Related Behavior and Circulating Levels of Corticosterone During Neophobic Tests of Anxiety

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