Histamine-induced modulation of nociceptive responses

Thoburn, Kathleen K.; Hough, Lindsay B.; Nalwalk, Julia W.; Mischler, Scott A.

doi:10.1016/0304-3959(94)90182-1

Cited by 65 publications

(41 citation statements)

References 29 publications

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“…Histamine, a pain-enhancing substance in the skin and spinal cord (Kajihara et al, 2010), reduces nociceptive transmission when injected directly into the brain (Glick and Crane, 1978;Chung et al, 1984;Bhattacharya and Parmar, 1985;Braga et al, 1992;Sibilia et al, 1992;Malmberg-Aiello et al, 1994;Thoburn et al, 1994). H 1 and H 2 receptors are thought to mediate this effect (Thoburn et al, 1994;Braga et al, 1996;Lamberti et al, 1996).…”

Section: Antinociceptive Profile For Brain Histaminementioning

confidence: 99%

“…H 1 and H 2 receptors are thought to mediate this effect (Thoburn et al, 1994;Braga et al, 1996;Lamberti et al, 1996). Related to pain relief, H 2 receptors in the brain are activated as part of opioid and nonopioid antinociceptive mechanisms , especially when stress elicits or enhances these responses (Nalwalk and Hough, 1995).…”

Section: Antinociceptive Profile For Brain Histaminementioning

confidence: 99%

“…The figure shows that: 1) the biphasic actions of systemically injected Thio can be replicated by microinjections of the same drug into the PAG, and 2) intracerebral HA injections in the PAG can closely mimic the effects of Thio, consistent with the known HA-releasing properties of this H 3 inverse agonist. Data are plotted: a, 15 min after Thio (MalmbergAiello et al, 1994); b, 40 min after Thio (Farzin et al, 2002); c, 10 min after intra-PAG Thio (Li et al, 1996); d, 5 min after intra-PAG HA (Thoburn et al, 1994). jpet.aspetjournals.org…”

Section: H 3 Rs In Models Of Chronic Painmentioning

confidence: 99%

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H₃ Receptors and Pain Modulation: Peripheral, Spinal, and Brain Interactions

Hough¹,

Rice²

2010

J Pharmacol Exp Ther

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Histamine H 3 receptors (H 3 Rs), distributed within the brain, the spinal cord, and on specific types of primary sensory neurons, can modulate pain transmission by several mechanisms. In the skin, H 3 Rs are found on certain A␤ fibers, and on keratinocytes and Merkel cells, as well as on deep dermal, peptidergic A␦ fibers terminating on deep dermal blood vessels. Activation of H 3 Rs on the latter in the skin, heart, lung, and dura mater reduces calcitonin gene-related peptide and substance P release, leading to anti-inflammatory (but not antinociceptive) actions. However, activation of H 3 Rs on the spinal terminals of these sensory fibers reduces nociceptive responding to lowintensity mechanical stimuli and inflammatory stimuli such as formalin. These findings suggest that H 3 R agonists might be useful analgesics, but these drugs have not been tested in clinically relevant pain models. Paradoxically, H 3 antagonists/ inverse agonists have also been reported to attenuate several types of pain responses, including phase II responses to formalin. In the periaqueductal gray (an important pain regulatory center), the H 3 inverse agonist thioperamide releases neuronal histamine and mimics histamine's biphasic modulatory effects in thermal nociceptive tests. Newer H 3 inverse agonists with potent, selective, and brain-penetrating properties show efficacy in several neuropathic and arthritis pain models, but the sites and mechanisms for these actions remain poorly understood. Histamine and PainHistamine, found throughout the body in both neuronal and non-neuronal sources, can modify pain transmission by actions at multiple receptors in the skin, spinal cord, and brain. Rapidly expanding information on the distribution and functions of H 3 receptors (H 3 Rs) and the recent development of new H 3 R ligands have heightened interest in the possible modulation of pain by H 3 R-acting drugs. The present article provides a short, integrative overview of relevant studies (for review see also Sander et al., 2008;Tiligada et al., 2009;Gemkow et al., 2009). Measuring Pain in the LaboratoryPain, which can be defined as the central representation of tissue-damaging stimuli with sensory-discriminative, motivational, and cognitive components (Besson and Chaouch, 1987), is readily understood by humans as a sensory experience. Ideally, evaluation of the pain-relieving properties of drugs should directly measure reductions in pain perception. Instead, assessment of analgesic drug action in nonverbal subjects relies heavily on measures of behavioral, often reflexive, responses. Because drugs can modify these responses (but not necessarily the underlying perceptions), results from pain testing in laboratory animals can be misleading. The present limitations of preclinical methodologies for identifying pain-relieving drugs have been discussed previously Vierck et al., 2008).Notwithstanding the limitations in state-of-the-art analgesic testing, many factors must be considered when evaluating

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Section: Antinociceptive Profile For Brain Histaminementioning

confidence: 99%

Section: Antinociceptive Profile For Brain Histaminementioning

confidence: 99%

Section: H 3 Rs In Models Of Chronic Painmentioning

confidence: 99%

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H₃ Receptors and Pain Modulation: Peripheral, Spinal, and Brain Interactions

Hough¹,

Rice²

2010

J Pharmacol Exp Ther

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“…Intracerebroventricular (ICV) injection of histamine at low doses induces hyperalgesia by acting on presynaptic receptors (H 3 receptors) whereas at high levels it elicits antinociception by acting on postsynaptic receptors (H 1 and H 2 receptors) (Malmberg-Aiello et al 1994;Brown et al 2001). ICV injection of H 1 and H 2 receptor antagonists into the periaqueductal gray has an antinociceptive effect (Thoburn et al 1994). Previously, Mojtahedin et al (2008) reported that ICV pre-treatment with mepyramine (H 1 -receptor antagonist) and famotidine (H 2 -receptor antagonist) prevented histamine-induced antinociception in the formalin test in rats.…”

Section: Discussionmentioning

confidence: 99%

Antinociceptive mechanisms of Bunium persicum essential oil in the mouse writhing test: role of opioidergic and histaminergic systems

Zendehdel¹,

Torabi²,

Hassanpour³

2015

Vet. Med.

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Bunium persicum (Boiss.) is an economically important medicinal plant growing wildly in arid regions in Iran. The fruit of B. persicum is widely used in traditional Iranian medicine to control colic pain and dysmenorrhoea. The aim of the current study was to determine antinociceptive mechanisms of B. persicum essential oil using an acetic acid-induced writhing test as a model of visceral pain and to determine the possible involvement of opioidergic, serotoninergic and histaminergic systems on antinociceptive mechanisms of B. persicum in male mice. In experiment 1, B. persicum was intraperitoneally (i.p.) injected (0.001, 0.01, 0.05, 0.1, 0.5 and 1%; 10 ml/kg) in Tween-80 (0.5%) and a writhing test served as a model of visceral pain. In experiments 2-5, opioidergic receptor antagonist (naloxone, 2 mg/kg), serotonergic receptor antagonist (cyproheptadine, 4 mg/kg), histamine H 1 -receptor antagonist (chlorpheniramine, 20 mg/kg) and histamine H 2 -receptor antagonist (cimetidine, 12.5mg/kg) injection was followed by B. persicum (0.01%; 10 ml/kg) and the writhing test response was measured for 30 min. According to the results, essential oil of B. persicum, administered i.p. (0.001, 0.01, 0.05, 0.1, 0.5, and 1%; 10 ml/kg) in Tween-80 (0.5%), elicited antinociceptive effects in a dose-dependent manner. Moreover, the antinociceptive effect of B. persicum was significantly attenuated by pre-treatment with naloxone, chlorpheniramine and cimetidine (P < 0.001). These results suggest that B. persicum-induced analgesia may be mediated via opioidergic and histamine H 1 and H 2 receptors.

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“…O receptor H 2 parece estar envolvido na antinocicepção 9 , enquanto o receptor H 1 está relacionado à ação pró-nociceptiva 8,10 . Antagonistas de receptor H 1 apresentam ação supraespinhal, localizada no núcleo dorsal da rafe ou ao redor da substância cinzenta periaquedutal 11 e atuam em receptores pré-sinápticos 8 . Antagonistas do receptor H 2 como a famotidina e lupitidina apresentaram ações antinociceptivas quando usadas por via sistêmica 12 .…”

Section: Introductionunclassified

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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Histamine-induced modulation of nociceptive responses

Cited by 65 publications

References 29 publications

H₃ Receptors and Pain Modulation: Peripheral, Spinal, and Brain Interactions

H₃ Receptors and Pain Modulation: Peripheral, Spinal, and Brain Interactions

Antinociceptive mechanisms of Bunium persicum essential oil in the mouse writhing test: role of opioidergic and histaminergic systems

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

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Histamine-induced modulation of nociceptive responses

Cited by 65 publications

References 29 publications

H3 Receptors and Pain Modulation: Peripheral, Spinal, and Brain Interactions

H3 Receptors and Pain Modulation: Peripheral, Spinal, and Brain Interactions

Antinociceptive mechanisms of Bunium persicum essential oil in the mouse writhing test: role of opioidergic and histaminergic systems

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

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H₃ Receptors and Pain Modulation: Peripheral, Spinal, and Brain Interactions

H₃ Receptors and Pain Modulation: Peripheral, Spinal, and Brain Interactions