Histamine Receptor Library from OTAVA
VAUGHAN - Dec 10, 2014 - Histamine is an important biogenic amine which exerts its biological effects through four distinct rhodopsin-like G protein-coupled receptors such as H1-, H2-, H3- and H4-receptors. Histamine receptors have been considered as attractive therapeutic targets.
H1-receptors mediate different biological properties of allergic responses and are involved in many pathological processes of allergy, including allergenic rhinitis, atopic dermatitis, conjunctivitis, urticaria, asthma, and anaphylaxis.
H2-receptors are mainly present on parietal cells located in the stomach lining, and responsible for regulating the levels of gastric acid, excess of which can result in gastroenteritis.
H3-receptors are implicated in the regulation of the synthesis and release of different neurotransmitters. The drugs targeted at histamine H3 receptors could be promising agents for treatment of neurodegenerative diseases such as Alzheimer and Parkinson's disease, epilepsy, drug abuse and several affective, appetite and sleeping disorders.
H4-receptors are mainly expressed in cells of the human immune system and mediate several effects on chemotaxis with numerous cell types. Promising preclinical studies underline their role as an attractive target in the treatment of inflammatory and autoimmune diseases.
OTAVA offers new Histamine Receptor Antagonist Library containing 1,295 compounds. For library design crystal structure of human histamine H1 receptor in complex with doxepin was used. On its basis, homology models of two other human histamine receptors (H3 and H4) have been built and taken for flexible docking. Receptor structures were validated with reference sets of active compounds obtained from ChEMBL database. The selection of compounds has been made with inspection of intermolecular hydrogen bonds with crucial active sites residues and application of the docking score cut-off filtering.
If your research is focused on the development of antihistamines, this targeted library is a good choice to start with.
More information about the Histamine Receptor Antagonist Library you can find on OTAVAs web-site www.otavachemicals.com.