Evidence for hypernociception induction following histamine H1 receptor activation in rodents

Malmberg-Aiello, P.; Lamberti, C.; Ipponi, Alessandra; Bartolini, Alessandro; Schunack, Walter

doi:10.1016/s0024-3205(98)00295-1

Cited by 61 publications

(32 citation statements)

References 20 publications

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“…Furthermore, IP injection of chlorpheniramine and ranitidine significantly increased the latency time to the beginning of the first writhe and also significantly decreased the number of writhes in acetic acid (1%) induced visceral pain in rats [13]. It has been reported that the activation of H 1 receptors by 2-(3-trifluoromethylphenyl)-histamine, a selective histamine H 1 receptor agonist not only prevents the antinociception induced by the H 1 receptor antagonist but also increased sensitivity to noxious stimuli in rodents [5]. Farzin and Nosrati reported (2007) that IP injection of (20 and 30 mg/kg) dexchlorpheniramine (H 1 receptor antagonist) had an antinociceptive effect in both phases of formalin-induced pain and at a dose of 10 mg/kg antagonized the hyperalgesia induced by intracerebroventricular injection of histamine-trifluoromethyltoluidine (histamine H 1 agonist) [28].…”

Section: Discussionmentioning

confidence: 99%

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The Effect of Histamine H1 Receptor Antagonists on the Morphine-Induced Antinociception in the Acute Trigeminal Model of Nociception in Rats

Khalilzadeh

Azarpey

Hazrati

2016

Asian J Pharm Clin Res

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Objective: In this study, the effect of different classes of histamine H 1 receptor antagonists (chlorpheniramine, cetirizine, and fexofenadine), µ opioid receptor agonist (morphine), and opioid receptor antagonist (naloxone) in separate and combined treatments were investigated on the acute trigeminal model of pain in rats.Methods: Eye wiping test used for induction of acute trigeminal pain by putting a drop of NaCl, 5 M solution (40 µl) on the corneal surface of the eye, and the number of eye wipes counted during the first 30 seconds.Results: Intraperitoneal injection of both chlorpheniramine and cetirizine at doses of 10 and 20 mg/kg significantly inhibited the acute trigeminal pain. However, fexofenadine did not change corneal pain response. Morphine at doses of 1.25, 2.5, and 5 mg/kg reduced eye wipe responses. Administration of both chlorpheniramine and cetirizine but not fexofenadine before morphine-enhanced morphine analgesic activity, also pretreatment of animals with naloxone inhibited morphine, chlorpheniramine, and cetirizine-induced analgesia in the acute corneal pain. Conclusion:Our results showed that chlorpheniramine as a histamine H 1 antagonist that efficiently Penetrates blood-brain barrier (BBB) and cetirizine with less penetration of BBB but not fexofenadine (an H 1 receptor antagonist with a negligible brain-accessibility) could induce analgesia in the acute corneal pain via opioidergic mechanism. Coadministration of morphine with chlorpheniramine or cetirizine could enhance its analgesic activity in the acute trigeminal model of pain in rats.

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Section: Discussionmentioning

confidence: 99%

“…The central histaminergic system plays an important role in the pain modulation. Histamine showed dual analgesic and pronociceptive roles in the central nervous system [4][5][6].…”

Section: Introductionmentioning

confidence: 99%

The Effect of Histamine H1 Receptor Antagonists on the Morphine-Induced Antinociception in the Acute Trigeminal Model of Nociception in Rats

Khalilzadeh

Azarpey

Hazrati

2016

Asian J Pharm Clin Res

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“…In the former, histamine H 1 and H 2 receptors are involved in the modulation of pain sensations. [15][16][17] In the peripheral nervous system, it is reported that pyrilamine (histamine H 1 receptor antagonist) and cimetidine (histamine H 2 receptor antagonist) show analgesic effects in the formalin test. 18) In addition, anti-histaminic drugs show antinociceptive effects on formalin-induced stimuli.…”

Section: Discussionmentioning

confidence: 99%

The Antinociceptive and Anti-inflammatory Action of the CHCl3-Soluble Phase and Its Main Active Component, Damnacanthal, Isolated from the Root of Morinda citrifolia

Okusada

Nakamoto

Nishida

et al. 2011

Biological & Pharmaceutical Bulletin

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“…Esse tipo de investigação traz correlação confiável sobre o comportamento doloroso em animais conscientes e não submetidos à restrição física. Entre os vários comportamentos estereotipados provocados pela formalina, a frequência de elevação da pata tem sido amplamente utilizada 14,15,18-20,23-25. A maior parte dos estudos sobre os efeitos analgésicos de antagonistas de receptores da histamina tem focalizado os efeitos centrais produzidos 8,12,[26][27][28] . Estudando o efeito sistêmico de diferentes antagonistas de receptor H 2 , a lupitidina e famotidina apresentaram efeito analgésico, enquanto que a ranitidina não apresentou efeito analgésico em modelo de dor somática ou visceral 12 .…”

Section: Discussionunclassified

Efeito analgésico de antagonistas do receptor da histamina H2 em modelo de dor provocada por formalina em ratos

Fernanda¹,

Ashmawi²,

Palmeira³

et al. 2011

Rev. dor

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Rev Dor. São Paulo, 2011 jul-set;12(3):240-4 RESUMO JUSTIFICATIVA E OBJETIVOS: Antagonistas de receptor de histamina apresentam efeitos sobre a dor. Antagonistas de receptor H 1 apresentam efeito analgésico local, o papel de antagonistas de receptor H 2 sobre a dor no sistema nervoso periférico ainda não está claro. Esse estudo teve como objetivo avaliar os efeitos de diferentes antagonistas H 2 sobre a dor induzida pela administração de formalina na pata de ratos. MÉTODO: Foram estudados ratos machos divididos em grupos que receberam formalina na pata e diferentes antagonistas de receptor H 2 -ranitidina, cimetidina e loxtidina, injetados na pata em diferentes concentrações (0,05 μmol, 0,25 μmol ou 1 μmol SUMMARY BACKGROUND AND OBJECTIVES:Histamine receptor antagonists affect pain perception. H1 receptor antagonists present local analgesic effect, but the role of H2 receptor antagonists on pain in the peripheral nervous system is not clear yet. This study aimed at evaluating the effects of different H2 receptor antagonists on pain induced by formalin paw injection in rats. METHOD: Male rats were studied and divided into groups that received formalin and different H2 receptor antagonists -ranitidine, cimetidine and loxtidine, injected in the paw at different concentrations (0.05 mol, 0.25 mol or 1 mol). The number of flinches was evaluated during 45 minutes. RESULTS: Loxtidine inhibited the number of flinches in both phases of the test with the three different concentrations. Ranitidine decreased the number of flinches in phase II as from 0.25 mol. Cimetidine did not affect pain behavior. CONCLUSION: According to the results of this study, some H2 receptor antagonists presented local analgesic effects, which seem to be drug-related and not pharmacological class-specific.

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Evidence for hypernociception induction following histamine H1 receptor activation in rodents

Cited by 61 publications

References 20 publications

The Effect of Histamine H1 Receptor Antagonists on the Morphine-Induced Antinociception in the Acute Trigeminal Model of Nociception in Rats

The Effect of Histamine H1 Receptor Antagonists on the Morphine-Induced Antinociception in the Acute Trigeminal Model of Nociception in Rats

The Antinociceptive and Anti-inflammatory Action of the CHCl3-Soluble Phase and Its Main Active Component, Damnacanthal, Isolated from the Root of Morinda citrifolia

Efeito analgésico de antagonistas do receptor da histamina H2 em modelo de dor provocada por formalina em ratos

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