HISTAMINE SUBTYPE 3 RECEPTOR ANTAGONISTS: CURRENT STATUS WITH FUTURE PROSPECTS IN DRUG DISCOVERY AND DRUG DEVELOPMENT

摘要

The histamine H3 receptor is an G protein-coupled receptor that regulates neurotransmission in the central nervous system and plays a major role in cognitive and homeostatic functions. The third histamine receptor was discovered in 1983 by a traditional pharmacological approach, consisting of assessing the inhibitory effect of histamine on its own release from depolarized rat brain slices. Histamine H3 receptors are found mostly in central nervous system also to some extent in peripheral tissues and involved in the regulation of release of various neurotransmitters in brain. They have been implicated in diverse potential therapeutic applications such as sleep wake disorders, attention-deficient hyperactivity disorder, epilepsy, cognitive impairment and obesity. This review is aimed to provide an overview of marketed preparations and also experimental H3 receptor antagonists under pipeline of drug discovery and development