Antiinflammatory and antinociceptive effects of the selective histamine H4-receptor antagonists JNJ7777120 and VUF6002 in a rat model of carrageenan-induced acute inflammation

Coruzzi, Gabriella; Adami, Maristella; Guaita, Elena; Esch, Iwan J. P. de; Leurs, Rob

doi:10.1016/j.ejphar.2007.02.026

Cited by 122 publications

(104 citation statements)

References 24 publications

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“…These results, indicating the involvement of neuronal H4 receptors in acute thermal antinociception, are in agreement with previous studies reporting the decrease in mechanical hyperalgesia produced by VUF 8430 in a model of neuropathic pain (Smith et al, 2007). However, in contrast with our findings, it has been observed that the systemic administration of the H4 antagonists JNJ7777120 and JNJ 10191584 exhibited anti-hyperalgesic activity in different models of inflammatory pain and anti-allodynic effects in models of neuropathic pain (Coruzzi et al, 2007;Hsieh et al, 2010). This discrepancy might be explained considering that this antihyperalgesic effect is obtained following systemic administration of the H4 antagonists and, as stated by the authors, it appears to be secondary to the anti-inflammatory activity induced by the antagonism of the H4 receptor on immune system cells.…”

Section: Discussioncontrasting

confidence: 57%

Pleiotropic effect of histamine H4 receptor modulation in the central nervous system

2013

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a b s t r a c tThe histamine H4 receptor (H4R) is expressed primarily on cells involved in inflammation and immune responses. Recently, it has been reported the functional expression of H4R within neurons of the central nervous system, but their role has been poorly understood. The present study aimed to elucidate the physiopathological role of cerebral H4R in animal models by the intracerebroventricular administration of the H4R agonist VUF 8430 (20e40 mg per mouse). Selectivity of results was confirmed by the prevention of the effects produced by the H4R antagonist JNJ 10191584 (3e9 mg/kg p.o.). Neuronal H4R activation induced acute thermal antinociception, indicating that neuronal histamine H4R might be involved in the production of antinociception in the absence of an inflammatory process. An anxiolyticlike effect of intensity comparable to that exerted by diazepam, used as reference drug, was produced in the lightedark box test. VUF 8430 reversed the scopolamine-induced amnesia in the passive avoidance test and showed anorexant activity in food deprived mice. Conversely, the H4R activation did not modify the immobility time in the tail suspension test. Rotarod performance test was employed to demonstrate that the effects observed following the administration of VUF 8430 and JNJ 10191584 were not due to impaired motor function of animals. Furthermore, both compounds did not alter spontaneous mobility and exploratory activity in the hole board test. These results show the antinociceptive, antiamnesic, anxiolytic and anorexant effects induced by neuronal H4R agonism, suggesting that H4 modulators may have broader utility further the control of inflammatory and immune processes.

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Section: Discussioncontrasting

confidence: 57%

Pleiotropic effect of histamine H4 receptor modulation in the central nervous system

2013

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“…The administration of JNJ dose-dependently reduced the ear edema and the scratching response [46]. In a rat model of carrageenan-induced acute inflammation, H 4 R antagonists decreased the formation of edema [28] and, in the early phase, significantly reduced the hyperalgesia consequent to thermal stimulation, controlling peripheral nociceptive pathway [47]. Histamine H 4 R is functionally expressed in cells of immune system [48] antagonists.…”

Section: Discussionmentioning

confidence: 99%

Role of histamine H 4 receptor ligands in bleomycin-induced pulmonary fibrosis

Lucarini

Pini

Rosa

et al. 2016

Pharmacological Research

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Use policyThe full-text may be used and/or reproduced, and given to third parties in any format or medium, without prior permission or charge, for personal research or study, educational, or not-for-prot purposes provided that:• a full bibliographic reference is made to the original source • a link is made to the metadata record in DRO • the full-text is not changed in any way The full-text must not be sold in any format or medium without the formal permission of the copyright holders.Please consult the full DRO policy for further details. This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. The results here reported clearly demonstrated that H 4 R ligands have a beneficial effect in a model of lung fibrosis in the mouse, thus indicating that H 4 R antagonists or inverse agonists could be a novel therapeutic strategy for lung inflammatory diseases.4

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“…Inflammation was expressed as the percentage change in paw volume. [31] Compounds under study were administered intragastrically (i.g.) in a volume of 10 mL kg À1 immediately before carrageenan injection.…”

Section: Methodsmentioning

confidence: 99%

Multitarget Drugs: Synthesis and Preliminary Pharmacological Characterization of Zileuton Analogues Endowed with Dual 5‐LO Inhibitor and NO‐Dependent Activities

et al. 2010

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Antiinflammatory and antinociceptive effects of the selective histamine H4-receptor antagonists JNJ7777120 and VUF6002 in a rat model of carrageenan-induced acute inflammation

Cited by 122 publications

References 24 publications

Pleiotropic effect of histamine H4 receptor modulation in the central nervous system

Pleiotropic effect of histamine H4 receptor modulation in the central nervous system

Role of histamine H 4 receptor ligands in bleomycin-induced pulmonary fibrosis

Multitarget Drugs: Synthesis and Preliminary Pharmacological Characterization of Zileuton Analogues Endowed with Dual 5‐LO Inhibitor and NO‐Dependent Activities

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