Histaminergic Pharmacology Modulates the Analgesic and Antiedematogenic Effects of Spinally Injected Morphine

Stein, Taciane; Souza-Silva, Eduardo; Mascarin, Lucas; Eto, Carolina; Fin, Franci Ellen; Tonussi, Carlos Rogério

doi:10.1213/ane.0000000000001326

Cited by 11 publications

(6 citation statements)

References 46 publications

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“…Histamine has been implicated in pain modulation, augmenting the transmission of nociceptive impulses; considerable evidence indicates that several H 1 blockers are indeed analgesic agents (McHugh and McHugh, 2000;Mobarakeh et al, 2000;Sakurada et al, 2004). Recent data indicate that cetirizine potentiates the analgesic and antiedematogenic effects of morphine (Stein et al, 2016), suggesting an unexplored use for classic antihistamines in pain relief.…”

Section: Histaminergic Regulation Of the Signaling Of Other Receptorsmentioning

confidence: 99%

Current Knowledge and Perspectives on Histamine H₁and H₂Receptor Pharmacology: Functional Selectivity, Receptor Crosstalk, and Repositioning of Classic Histaminergic Ligands

Monczor

Fernández

2016

Mol Pharmacol

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H 1 and H 2 histamine receptor antagonists, although developed many decades ago, are still effective for the treatment of allergic and gastric acid-related conditions. This article focuses on novel aspects of the pharmacology and molecular mechanisms of histamine receptors that should be contemplated for optimizing current therapies, repositioning histaminergic ligands for new therapeutic uses, or even including agonists of the histaminergic system in the treatment of different pathologies such as leukemia or neurodegenerative disorders. In recent years, new signaling phenomena related to H 1 and H 2 receptors have been described that make them suitable for novel therapeutic approaches. Crosstalk between histamine receptors and other membrane or nuclear receptors can be envisaged as a way to modulate other signaling pathways and to potentiate the efficacy of drugs acting on different receptors. Likewise, biased signaling at histamine receptors seems to be a pharmacological feature that can be exploited to investigate nontraditional therapeutic uses for H 1 and H 2 biased agonists in malignancies such as acute myeloid leukemia and to avoid undesired side effects when used in standard treatments. It is hoped that the molecular mechanisms discussed in this review contribute to a better understanding of the different aspects involved in histamine receptor pharmacology, which in turn will contribute to increased drug efficacy, avoidance of adverse effects, or repositioning of histaminergic ligands.

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Section: Histaminergic Regulation Of the Signaling Of Other Receptorsmentioning

confidence: 99%

Current Knowledge and Perspectives on Histamine H₁and H₂Receptor Pharmacology: Functional Selectivity, Receptor Crosstalk, and Repositioning of Classic Histaminergic Ligands

Monczor

Fernández

2016

Mol Pharmacol

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“…The pathogenesis of RA can be influenced by the inflammatory potentials of spinal cord 8 . Stimuli such as mechanical trauma, pH changes, presence of inflammatory mediators, can trigger a process called neurogenic inflammation 9 , which reflects the release of neurotransmitters from the primary afferent, such as sP and CGRP 10 , which enhance peripheral inflammation. One study has inferred that a sensitive nerve contralateral to arthritis induction, leads to action potentials towards the periphery; also observed that animals induced to an inflammatory process by FCA, presented greater spontaneous antidromic activity when compared to a control group.…”

Section: Discussionmentioning

confidence: 99%

Low-level laser therapy in periarticular morphological aspects of the knee of Wistar rats in rheumatoid arthritis model

Neves¹,

Tavares²,

Retameiro³

et al. 2020

Brazilian Journal of Pain

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BACKGROUND AND OBJECTIVES: The deleterious effects of rheumatoid arthritis on periarticular tissues have not yet been fully elucidated. Therefore, the search for treatments that can modulate the inflammatory profile and tissue remodeling is pertinent. The present study evaluated the effects of low-level laser therapy (LLLT) on the morphology of periarticular tissues and synovial membrane of rats in a rheumatoid arthritis model. METHODS: Sixty-four male rats were divided into acute (7 days) and chronic (28 days) inflammatory periods, with four groups (n=8) each, being: CG (control group), LG (lesion group), CLaG (laser control group) and LLaG (laser lesion group). The animals of the lesion groups received two inoculations of Freund's Complete Adjuvant at a concentration of 50µL, the first at the base of the tail, and the second at the right knee. The animals in the control groups were injected with isotonic sodium chloride solution. The ClaG and LLaG were treated with 660nm LBI, 5J/cm 2 in the right knee. After the experimental period, the animals were euthanized, and the knees were processed for light microscopy. RESULTS: The CG and CLaG morphological analysis had normal aspects. The LG showed synovitis, femur, and tibia with changes in the periosteum, with inflammatory cells and bone modifications. In the LLaG, the synovial membrane showed signs of improvement. Bone tissue in the chronic period showed morphological aspects, denoting tissue remodeling. Low-level laser therapy in periarticular morphological aspects of the knee of Wistar rats in rheumatoid arthritis model Laser de baixa intensidade nos aspectos morfológicos periarticulares do joelho de ratos Wistar em modelo de artrite reumatoide

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“…Repositioning antihistaminergic ligands seems a promising idea given that histamine exerts a variety of actions throughout the body and that histamine H 1 and H 2 receptors are ubiquitously expressed. In this sense, novel clinical applications for histamine H 1 receptor antagonists/inverse agonists are currently being studied for the management of different pathological situations, such as inflammatory-related conditions (in combination with glucocorticoids) (Zappia et al, 2015), analgesia (Stein et al, 2016) or neurodegenerative and sleep disorders (Kim and Song, 2017;Krystal, 2015). In the same way, evidence for anti-cancer effects of the histamine H 2 receptor inverse agonist cimetidine has been reported in various types of neoplasias, including glioblastoma, cholangiocarcinoma, malignant melanoma, renal cell carcinoma, colorectal and gastric cancer (Dana et al, 2017;Pantziarka et al, 2014).…”

Section: Discussionmentioning

confidence: 99%

Involvement of histamine H1 and H2 receptor inverse agonists in receptor's crossregulation

Nebreda

Zappia

González

et al. 2019

European Journal of Pharmacology

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Histamine [2-(4-Imidazolyl)-ethylamine] modulates different biological processes, through histamine H 1 and H 2 receptors, and their respective blockers are widely used in treating allergic and gastric acid-related disorders. Histamine H 1 and H 2 receptor crossdesensitization and cointernalization induced by its agonists have been previously described. In this study, we show how this crosstalk determines the response to histamine H 1 and H 2 receptor inverse agonists and how histamine H 1 and H 2 receptor inverse agonists interfere with the other receptor's response to agonists. By desensitization assays we demonstrate that histamine H 1 and H 2 receptor inverse agonists induce a crossregulation between both receptors. In this sense, the histamine H 1 receptor inverse agonists desensitize the cAMP response to amthamine, a histamine H 2 receptor agonist. In turn, histamine H 2 receptor inverse agonists interfere with histamine

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Histaminergic Pharmacology Modulates the Analgesic and Antiedematogenic Effects of Spinally Injected Morphine

Cited by 11 publications

References 46 publications

Current Knowledge and Perspectives on Histamine H₁and H₂Receptor Pharmacology: Functional Selectivity, Receptor Crosstalk, and Repositioning of Classic Histaminergic Ligands

Current Knowledge and Perspectives on Histamine H₁and H₂Receptor Pharmacology: Functional Selectivity, Receptor Crosstalk, and Repositioning of Classic Histaminergic Ligands

Low-level laser therapy in periarticular morphological aspects of the knee of Wistar rats in rheumatoid arthritis model

Involvement of histamine H1 and H2 receptor inverse agonists in receptor's crossregulation

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Histaminergic Pharmacology Modulates the Analgesic and Antiedematogenic Effects of Spinally Injected Morphine

Cited by 11 publications

References 46 publications

Current Knowledge and Perspectives on Histamine H1and H2Receptor Pharmacology: Functional Selectivity, Receptor Crosstalk, and Repositioning of Classic Histaminergic Ligands

Current Knowledge and Perspectives on Histamine H1and H2Receptor Pharmacology: Functional Selectivity, Receptor Crosstalk, and Repositioning of Classic Histaminergic Ligands

Low-level laser therapy in periarticular morphological aspects of the knee of Wistar rats in rheumatoid arthritis model

Involvement of histamine H1 and H2 receptor inverse agonists in receptor's crossregulation

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Current Knowledge and Perspectives on Histamine H₁and H₂Receptor Pharmacology: Functional Selectivity, Receptor Crosstalk, and Repositioning of Classic Histaminergic Ligands

Current Knowledge and Perspectives on Histamine H₁and H₂Receptor Pharmacology: Functional Selectivity, Receptor Crosstalk, and Repositioning of Classic Histaminergic Ligands