Histamine H3 Receptor Antagonists: Preclinical Promise for Treating Obesity and Cognitive Disorders
Mol. Interv. 2006 6: 77-88.
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Since the original description of the histamine H3 receptor as a presynaptic autoreceptor that inhibits histamine release, there has been considerable effort to develop potent and selective H3 receptor antagonists for the potential treatment of a variety of disorders affecting cognition (Attention Deficit Hyperactivity Disorder, Alzheimer Disease, and schizophrenia), sleep (hypersomnia and narcolepsy), and homeostasis (obesity). We review some of the preclinical considerations, from both an H3 receptor biology as well as a more general drug discovery perspective, that need to be taken into account in developing effective H3 receptor antagonists for the treatment of these diseases.