Histamine H3 Receptors
Histamine H3 receptors are Gαi/o-protein-coupled receptors first cloned in 1999. H3 receptors are expressed at high levels on histaminergic neurons in the central nervous system, particularly in the basal ganglia, cortex, hippocampus and strial area. They are expressed in the periphery at lower densities in the gastrointestinal, bronchial and cardiovascular systems.
H3 receptors are thought to function as presynaptic autoreceptors and their activation stimulates the negative feedback mechanism that reduces central histaminergic activity. These receptors have displayed heterogeneity in binding and functional studies, suggesting multiple subtypes. In rats, three H3 receptor subtypes have been identified and they all vary in the length of the third extracellular loop, have distinct CNS localization and differentially couple to adenylyl cyclase and MAPK signaling pathways.
H3 receptors have multiple functions including roles in cognition, sleep-wake status, energy homeostasis regulation and inflammation. Activation of these receptors can inhibit histamine, dopamine, serotonin, noradrenalin and acetylcholine release and they participate in control of neurogenic inflammation through local-neuron feedback loops. Furthermore, H3 receptor activation increases antigen-presenting cell capacity.
H3 receptors are thought to have pathophysiological relevance and are involved in cognitive impairment, seizures and possibly metabolic syndrome. The human gene encoding this receptor is localized to chromosome 20q13.33.View all products for Histamine H3 Receptors »
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Literature for Histamine H3 Receptors
A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:
- Rhodopsin-like Receptors
- Secretin-like Receptors
- Glutamate Receptors
- Frizzled Receptors
- GPCR Signaling
This review provides a synopsis of the different histamine receptor subtypes and the ligands that act upon them. Compounds available from Tocris are listed.Download PDF | View all reviews
Written by Alan Palmer and updated in 2015, this poster summarizes structural and functional changes observed in the progression of Alzheimer's disease (AD), as well as classic AD drug targets. The hypotheses behind the neurobiology of AD are discussed alongside the different stages in disease progression. Compounds available from Tocris are listed.Request copy | Download PDF | View all posters
Written by Peter Barnes, this poster highlights key pathways in the development of asthma. Special focus is given to new therapies used to treat asthma, including those currently in clinical development; treatment pathways include lipid mediator inhibitors, cytokine modulators and mast cell-directed therapies. Compounds available from Tocris are listed.Request copy | View all posters