Histamine H3 Receptor Antagonists Small Molecules and Peptides

Histamine H₃ receptors are G_αi/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 ...