Delineation of receptor-ligand interactions at the human histamine H ₁ receptor by a combined approach of site-directed mutagenesis and computational techniques - or - how to bind the H₁ receptor

Histamine H₁ antagonists or "antihistamines" are one of the most prescribed drug families in Western countries. They exert their effect by binding to the histamine H₁ receptor, a receptor belonging to the class of rhodopsin-like G protein-coupled receptors (GPCRs). In this review, the binding of ligands to the human histamine H₁ receptor with respect to site-directed mutagenesis studies and molecular modeling techniques is described. The ligands described include agonists (histamine and histaprodifens), a stereoselective partial agonist (lisuride), and selected inverse agonists (mepyramine, acrivastine and triprolidine).