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).
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
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Review
MeSH terms
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Computational Biology / methods*
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Histamine Agonists / chemistry
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Histamine Agonists / pharmacology
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Histamine Agonists / therapeutic use
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Histamine H1 Antagonists / chemistry
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Histamine H1 Antagonists / pharmacology
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Histamine H1 Antagonists / therapeutic use
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Humans
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Ligands*
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Mutagenesis, Site-Directed / drug effects
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Mutagenesis, Site-Directed / physiology
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Receptors, Histamine H1 / chemistry
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Receptors, Histamine H1 / genetics*
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Receptors, Histamine H1 / metabolism
Substances
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Histamine Agonists
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Histamine H1 Antagonists
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Ligands
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Receptors, Histamine H1