Histamine H3receptor antagonists

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Abstract
The histamine H3 receptor provides a negative feedback mechanism for the release and synthesis of histamine. On non-histaminergic neurones the H3 receptor regulates the release of many other neurotransmitters. Blockade of stimulated H3 receptors results in the release of endogenous neurotransmitters. Possible indications for a histamine H3 receptor antagonist include attention-deficit hyperactivity disorder (ADHD), epilepsy, Alzheimer’s disease, narcolepsy, epilepsy, obesity, schizophrenia and respiratory diseases such as allergic rhinitis. Current H3 receptor antagonists fall into two classes, imidazole-containing and non-imidazole compounds, with there being far more examples of the former. The development of imidazole antagonists has produced the compound GT-2331 (Perceptin™, Gliatech), which has successfully passed early stage clinical trials. The search for non-imidazole antagonists is a burgeoning area, which may profit from the recent cloning of a human H3 receptor.