Smit M J, Hoffmann M, Timmerman H, Leurs R
Mount Sinai Medical Center, Mount Sinai School of Medicine, Department of Pharmacology, New York, New York, USA.
Clin Exp Allergy. 1999 Jul;29 Suppl 3:19-28.
With cloning of the gene encoding the histamine H1 receptor, a new area of histamine research has become reality. Finally, it seems feasible to study the target of the therapeutically important clans of antihistamine. Expression of the genes in mammalian cells allows detailed investigations of the various signal transduction routes of the histamine H1 receptor. Moreover, using molecular biological techniques, it is now possible to investigate ligand receptor interaction at the molecular level. Studies with mutant H1 receptors have shown that H1 antagonists bind to a specific amino acid residues in TM3 and 5. It is expected that these new developments will provide much fundamental knowledge on the ligand interaction with the H1 receptor.