title: Delineation of receptor-ligand interactions at the human histamine H1 receptor by a combined approach of site-directed mutagenesis and computational techniques - or - how to bind the H1 receptor.
abstract: Histamine H(1) antagonists or "antihistamines" are one of the most prescribed drug families in Western countries. They exert their effect by binding to the histamine H(1) 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 H(1) 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).
authors.affiliation: Leiden/Amsterdam Center for Drug Research, Division of Medicinal Chemistry, Faculty of Science, Vrije Universiteit Amsterdam, The Netherlands.
authors.forename: Aldo
authors.initials: A
authors.lastname: Jongejan
authors.forename: Rob
authors.initials: R
authors.lastname: Leurs
mesh_terms: D019295:Computational Biology / Q000379:methods*; D017442:Histamine Agonists / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D006634:Histamine H1 Antagonists / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D008024:Ligands; D016297:Mutagenesis, Site-Directed / Q000187:drug effects / Q000502:physiology; D011969:Receptors, Histamine H1 / Q000737:chemistry / Q000235:genetics* / Q000378:metabolism
chemical_list: D017442:Histamine Agonists; D006634:Histamine H1 Antagonists; D008024:Ligands; D011969:Receptors, Histamine H1