Histamine GPCR Assays
Background of Histamine Receptors
Histamine is a bioactive amine that has been considered a key player in the allergic response. Histamine receptors are a group of 7-transmembrane receptors that mediate cellular responses to the biogenic amine histamine. Encoded by up to 1000 genes, histamine receptors mediate a variety of physiologic responses.
Fig.1. Histamine receptor structure and function. (Mandola, 2019)
Distribution and Function of Histamine Receptors
The wide distribution of histamine receptors in the body has been demonstrated. One or more receptors expressed at significant levels can be detected in neurons, smooth muscle (blood vessels, stomach, and bronchi), blood, heart, immune system, and endocrine system. H1 receptor mediates the postsynaptic effects of histamine within the CNS. The activation of the H2 receptor leads to activation of cAMP-dependent and -independent pathways. The activation of the H3 receptor relates to enhanced Ca2+ influx, MAP kinase, and inhibition of cAMP. H4 receptor activation induces calcium mobilization and the regulation of other non-hematopoietic systems.
Subtypes and Mechanisms of Histamine Receptors
Currently, there are four subtypes of histamine receptors have been identified, including the H1 receptor, H2 receptor, H3 receptor, and H4 receptor. All four of these subtypes are involved in some degree of inflammation and thus have been important targets for clinical research.
| Receptor | Gene | Mechanism | Agonists | Antagonists |
| H1 receptor | HRH1 |
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| H2 receptor | HRH2 |
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| H3 receptor | HRH3 |
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| H4 receptor | HRH4 |
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Assay List of Histamine Receptors
Creative Biolabs can provide a range of assays of histamine receptors. You can choose the assay in the list or contact us for more information:
Published Data
| Paper Title | Histamine, histamine receptors, and neuropathic pain relief |
| Journal | British Journal of Pharmacology |
| Published | 2020 |
| Abstract | Histamine regulates various physiological and pathological processes through distinct histamine H1, H2, H3, and H4 receptors. Over the past few decades, H3 receptors and H4 receptors have been reported to be involved in the modulation of neuropathic pain. However, recent data suggest that the pharmacological response of histamine receptors and their underlying signaling properties are influenced by multiple factors leading to differential responses to neuropathic pain. This article addresses the role of histamine and the role of four histamine receptors in the response to neuropathic pain. In addition, we also investigated the underlying mechanism of histamine-mediated analgesia. |
| Result |
Over the past few decades, studies have shown that neurons expressing H3 receptors may provide promising therapeutic approaches for controlling mechanical and cold hypersensitivity in peripheral neuropathy. Centrally penetrant H2 receptor antagonists are useful in the treatment of neuropathic pain because of their analgesic effects and metabolic stability. Therefore, an in-depth understanding of the interactions between histaminergic signaling pathway molecules and histamine receptors could lead to new pharmacological targets to improve neuropathic pain. Furthermore, the analgesic activity of H4 receptor stimulation for neuropathic pain is regulated by multiple factors such as MAPK/ERK signaling in DRG, spinal cord, and sciatic nerve neurons.
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Fig.2. Diagram illustrating histamine receptor signaling-Gi pathway. (Obara, et al., 2022)
References
- Mandola, A.; et al. Histamine, histamine receptors, and anti-histamines in the context of allergic responses. LymphoSign Journal. 2019, 6(2): 35-51.
- Obara, I.; et al. Histamine, histamine receptors, and neuropathic pain relief. British Journal of Pharmacology. 2020, 177(3): 580-599.
