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.
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).
Jongejan
Aldo
A
Leiden/Amsterdam Center for Drug Research, Division of Medicinal Chemistry, Faculty of Science, Vrije Universiteit Amsterdam, The Netherlands.
Leurs
Rob
R
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
D017442:Histamine Agonists; D006634:Histamine H1 Antagonists; D008024:Ligands; D011969:Receptors, Histamine H1