Histamine H₃ receptor antagonists

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.

• allergic rhinitis
• Alzheimer’s disease
• attention-deficit hyperactivity disorder
• epilepsy
• GT-2331
• histamine H3 antagonist
• histamine
• imidazole
• narcolepsy
• obesity
• schizophrenia