Histamine H3 Receptors

Supporting information

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.

To view external sources of pharmacological information for Histamine H3 Receptors, please click here: IUPHAR Receptor Code and BJP Guide

View all products for Histamine H3 Receptors »
Species Gene Symbol Gene Accession No. Protein Accession No.
Human HRH3 NM_007232 Q9Y5N1
Mouse Hrh3 NM_133849 P58406
Rat Hrh3 NM_053506 Q9QYN8

Literature for Histamine H3 Receptors

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