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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 H 1 Receptor
Author(s) -
Jongejan Aldo,
Leurs Rob
Publication year - 2005
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200400998
Subject(s) - g protein coupled receptor , chemistry , histamine receptor , histamine , histamine h4 receptor , stereochemistry , agonist , receptor , inverse agonist , histamine h3 receptor , ligand (biochemistry) , histamine h2 receptor , rhodopsin , histamine h1 receptor , mutagenesis , binding site , partial agonist , pharmacology , biochemistry , antagonist , biology , mutation , retinal , gene
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 histapro difens), a stereoselective partial agonist (lisuride), and selected inverse agonists (mepyramine, acrivastine and triprolidine).