Obesity
Divya Vohora in The Third Histamine Receptor, 2008
As indicated earlier, histamine has been shown to have a demonstrable effect on reducing food consumption and weight gain. Histamine is known to be able to activate all four subtypes (H1, H2, H3, and H4) of the G-protein-coupled histamine receptors, each of which exhibits distinct expression patterns as well as molecular, pharmacological, and signaling properties [25]. The reader is referred to Chapter 4 for further description of the properties of these receptors. The two most prominent histamine receptors involved in feeding/weight regulation based on scientific data to date are the H1 and H3 receptors, and for the purposes of this discussion and to illustrate several rather simple concepts in an otherwise very complex system, the role of these two histamine receptors will be elucidated here, again keeping in mind that the interaction of other neurotransmitters and neuronal pathways may influence the effects mediated by these receptors.
Pharmacotherapy of Neurochemical Imbalances
Sahab Uddin, Rashid Mamunur in Advances in Neuropharmacology, 2020
There are four subtypes of histamine receptors—H1, H2, H3, and H4 (Table 22.6). They are widely scattered centrally and in periphery. All four types of histamine receptors are GPCRs. H1 and H2 receptors are post-synaptic, located on neuroeffector junction. Unlike H1 and H2 receptors, H3 receptors are presynaptic, and prevent secretion of histamine and other transmitters via a G-protein. H4 receptors are located on blood cells like eosinophils, neutrophils, and CD4 T cells. Of the four types, H1 and H2 receptors, agonists, and antagonists have been studied extensively for targets of drug research (Barrett et al., 2009; Nestler et al., 2009).
Targeting the Lungs with Therapeutic Aerosols
Hans Bisgaard, Chris O’Callaghan, Gerald C. Smaldone in Drug Delivery to the Lung, 2001
Histamine plays a central role in immunologic and anti-inflammatory responses, particularly in the immediate hypersensitivity response. Three subclasses of histamine receptors have been identified: H1, H2, and H3 receptors. H1 receptors are involved in mediating increased vascular permeability, pruritus, contraction of smooth muscle in the respiratory and gastrointestinal tracts, release of mediators of inflammation, and recruitment of inflammatory cells. Among other effects, H3 receptors mediate the negative feedback control of histamine synthesis and release and may play some defensive role against excess bronchoconstriction. H1 and H3 receptors are both found primarily in bronchial smooth muscle in the human respiratory tract (40).
The clinical relationship between histamine-1 receptor antagonists and risk of cancer: a systematic review and meta-analysis
Published in Expert Review of Anticancer Therapy, 2023
Elham Bakhtiari, Nasrin Moazzen, Amir Amirabadi, Hamid Ahanchian
Wide variety of mammalian cells express histamine receptor 1. One of these cells are cluster of differentiation 4+ T helper1 (Th1) lymphocytes. It predominantly expresses in H1 receptor (H1R), while H2 receptor (H2R) expresses more in CD4 + T helper2 lymphocytes. Effect of histamine in H1R is enhancing Th1- type response. However, attenuating of both Th1 and Th2 type responses will occur by H2R [29]. Natural killer cells produce high amounts of interferon gamma (IFN-ν) after recognizing malignant cells; augmenting Th1 type, and cytotoxic T lymphocyte response [30]. One suggestion may be suppressing Th1 response by antagonizing H1R and attenuating anti-cancer activity of natural killer (NK) cells [30]. Another possible pathway, which may involve histamine in carcinogenesis, is enhancing vascular endothelial growth factor (VEGF), one of proangiogenic cytokines. It can be due to overexpression of cyclooxygenase 2 (COX2) pathway and enhanced activity of histidine decarboxylase [31,32]. Some studies exhibit higher concentration of histamine and histidine decarboxylase in breast cancer tissue [33].
Current and emerging pharmacotherapy for pediatric allergic rhinitis
Published in Expert Opinion on Pharmacotherapy, 2021
Peter Valentin Tomazic, Doris Lang-Loidolt
Four types of histamine receptors have been identified. H1 and H2 receptors are present on a wide range of cells, stimulate both the early and late phase of an allergic response Second/third generation non-sedating H1 receptor antagonists are the antihistamines of choice to treat AR [43]. Cetirizine has been proven effective in numerous studies, being superior in effect of symptom reduction to loratadine compared to placebo given an excellent safety profile [44,45]. The anti-inflammatory effect of antihistamines was shown to be mediated via the NFkappa-ß pathway; however, the clinical relevance of this potential has not been studied [46]. Apart from its effect on the H1 receptor it also reduces pro-inflammatory cytokines (e.g. IL-4 and IL-8). Cetirizine is used as of 6 months of age and 2 years of age in the US and Europe, respectively. It is effective given 10 mg daily in two doses for rhinoconjunctivitis symptoms (age 6–12 years) and 5 mg daily against sneezing [45].
Impact of IL-1β and the IL-1R antagonist on relapse risk and survival in AML patients undergoing immunotherapy for remission maintenance
Published in OncoImmunology, 2021
Hanna Grauers Wiktorin, Ebru Aydin, Karin Christenson, Nuttida Issdisai, Fredrik B. Thorén, Kristoffer Hellstrand, Anna Martner
Histamine, which is the endogenous counterpart to HDC, has been ascribed multiple effects on the production of cytokines from immune and inflammatory cells (reviewed in[38]). Histamine has thus been shown to modulate the formation of tumor necrosis factor (TNF), IL-1, IL-6, IL-10, IL-12 and IL-17 by leukocytes.38,39 Effects of histamine on cytokine production are determined by the cellular distribution and expression of subtypes of histamine receptors and may additionally encompass indirect effects on receptor expression with ensuing effects of cytokine production.38,40 Although histamine is well known as a mediator of allergic inflammation, mainly via its vascular effects downstream of the histamine type 1 receptor, several studies also shown that histamine may dampen myeloid cell-induced inflammation.34,41,42 These anti-inflammatory actions of histamine, including reduced NOX2-dependent ROS formation and reduced production of IL-12, TNF and IL-1 by myeloid cells, are typically mediated via histamine-type 2 receptors.34,38,39,43 The suggested anti-inflammatory role of histamine is bolstered by results achieved in genetically histamine-deficient mice, which are characterized by markedly increased myeloid cell-related inflammation along with increased growth of inflammation-induced cancer.44
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