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
✍ Scribed by Aldo Jongejan; Rob Leurs
- Publisher
- John Wiley and Sons
- Year
- 2005
- Tongue
- English
- Weight
- 313 KB
- Volume
- 338
- Category
- Article
- ISSN
- 0365-6233
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✦ Synopsis
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 histapro difens), a stereoselective partial agonist (lisuride), and selected inverse agonists (mepyramine, acrivastine and triprolidine).